Ligand source activities (1 row/activity)



Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL2064011 209171 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170042 208548 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170045 208551 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170640 208571 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170231 208558 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL5081621 214756 0 None 4 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170045 208551 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170231 208558 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170635 208566 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170635 208566 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
101886248 114974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 114974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44426497 85735 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229006 85735 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170026 208539 0 None 48 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
3915 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
49799079 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5760 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
91933514 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170027 208540 0 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
44426495 85734 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229005 85734 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL5080181 214668 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
101886248 114974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 114974 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL1170026 208539 0 None 48 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
3915 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
49799079 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5760 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
91933514 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170027 208540 0 None 30 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL5075364 214370 0 None -2511 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064020 209180 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
122392665 165441 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release
ChEMBL 457 10 6 5 3.3 N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O 10.1021/acs.jmedchem.7b00882
CHEMBL4239035 165441 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release
ChEMBL 457 10 6 5 3.3 N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O 10.1021/acs.jmedchem.7b00882
17753143 85940 4 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL230034 85940 4 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430551 88004 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234305 88004 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170025 208538 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
44426475 144669 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL390834 144669 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL2064012 209172 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
71525749 136429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 136429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71525749 136429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 136429 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5080381 214681 0 None -47 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170025 208538 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170043 208549 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71768012 136452 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 136452 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71768012 136452 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 136452 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426496 142042 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387755 142042 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL2063898 209170 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
44430554 151269 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396031 151269 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430547 168859 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL438129 168859 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170029 208542 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
11252 770 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 770 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 770 39 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170034 208546 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O 10.1021/jm1003705
CHEMBL1170043 208549 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
8381 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL1170029 208542 0 None 29 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170034 208546 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(N)=O 10.1021/jm1003705
CHEMBL2064018 209178 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
89570392 136477 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 136477 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570392 136477 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 136477 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1169838 208537 0 None -6 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170433 208562 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
8381 1029 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 1029 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 1029 3 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL2064016 209176 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170433 208562 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170229 208556 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1169838 208537 0 None -6 2 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170229 208556 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
71566581 136504 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 136504 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170643 208573 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2064018 209178 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Partial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerPartial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
71566581 136504 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 136504 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170643 208573 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL5092449 215368 0 None 2 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170648 208576 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170648 208576 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5087237 215080 0 None -446 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.1c01174
CHEMBL1170437 208564 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170437 208564 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170638 208569 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170035 208547 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170638 208569 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at C3aR in human MDM cells assessed as Ca2+ responseAgonist activity at C3aR in human MDM cells assessed as Ca2+ response
ChEMBL None None None None 10.1016/j.bmcl.2015.10.038
CHEMBL1170638 208569 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170035 208547 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL2064014 209174 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2064019 209179 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL1170641 208572 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170641 208572 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170650 208577 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/jm1003705
CHEMBL5080234 214671 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170637 208568 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170650 208577 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170637 208568 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5085743 214986 0 None -51 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170030 208543 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170221 208554 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170223 208555 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886250 114975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 114975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
49799093 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5761 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1172879 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170030 208543 11 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170221 208554 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
44426472 85704 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228847 85704 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Antagonist activity at C3aRAntagonist activity at C3aR
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170223 208555 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886250 114975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 114975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
127036518 136375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 136375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127036518 136375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 136375 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
49799093 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
5761 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1172879 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5082686 214820 0 None -275 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC[C@@H](C)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL5093227 215417 0 None -99 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
127034744 136406 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735339 136406 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL1170438 208565 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170438 208565 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 208563 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 208563 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL2064017 209177 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerAgonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL1170636 208567 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170636 208567 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
71565510 136393 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 136393 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 136538 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 136538 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426463 86394 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL231405 86394 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
71565510 136393 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 136393 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 136538 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 136538 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170044 208550 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1173027 208589 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170639 208570 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170232 208559 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170639 208570 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
117634952 136534 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 136534 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170232 208559 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
117634952 136534 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 136534 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170044 208550 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5083558 214870 0 None 2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
71565582 136454 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 136454 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 136454 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 136454 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1173027 208589 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5078171 214539 0 None -436 2 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL5071478 214259 6 None -933 3 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
71566653 136430 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 136430 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566653 136430 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 136430 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170028 208541 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2021602 209130 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm1003705
CHEMBL2021602 209130 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm1003705
CHEMBL1170046 208552 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5085196 214955 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170046 208552 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5081287 214739 0 None 30 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064017 209177 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2064019 209179 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerPartial agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064013 209173 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL1170349 208560 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170349 208560 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL5092461 215370 0 None -2041 2 Human 4.2 pEC50 = 4.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.1c01174
71566654 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
9449 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
CHEMBL3736108 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assayAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release measured for 5 mins by Fluo-3 AM dye-based fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1021/acs.jmedchem.7b00882
71566654 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71566654 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 1005 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71565580 136484 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 136484 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5079833 214646 0 None -7 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL2064015 209175 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
71565506 136476 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 136476 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170220 208553 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565506 136476 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 136476 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 136355 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 136355 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 136355 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 136355 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5092578 215376 0 None -295 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1169603 208536 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL2064016 209176 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate readerAgonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as increase in intracellular calcium using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
44430549 151266 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396030 151266 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL1169603 208536 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
CHEMBL1170220 208553 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565580 136484 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 136484 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL2064021 209181 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay
ChEMBL None None None None 10.1021/jm201609k
117637102 136530 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 136530 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117637102 136530 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 136530 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assayAgonist activity at C3aR in human MDM cells assessed as inhibition of C3a-induced Ca2+ response measured for 60 secs by fluorescence assay
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL5076900 214468 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C3aR expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.1c01174
CHEMBL1170230 208557 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170230 208557 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170042 208548 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None None 10.1021/jm1003705
8384 1113 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 1113 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 1113 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL2064013 209173 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
10595 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL2064012 209172 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
155525092 170940 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4455385 170940 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155535693 172069 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 486 10 5 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(F)cc2)c2ccc(F)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4472149 172069 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 486 10 5 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(F)cc2)c2ccc(F)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155558856 174815 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 478 12 5 4 3.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(Cc2ccccc2)Cc2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4562412 174815 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 478 12 5 4 3.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(Cc2ccccc2)Cc2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
101886254 114966 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 114966 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
101886249 114967 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 114967 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL2064019 209179 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate readerAntagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064021 209181 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None None 10.1021/jm201609k
101886249 114967 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 114967 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
155535683 172071 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472196 172071 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155554899 174340 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551058 174340 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
3529 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
5311120 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL389348 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
101886254 114966 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 114966 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
127035774 136437 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ responseAntagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ response
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 136437 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ responseAntagonist activity against human C3aR expressed in rat RBL-2H3 cells assessed as inhibition of C3a-induced Ca2+ response
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
3529 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
3529 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 3517 9 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
155535683 172071 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472196 172071 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)sc1C(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155554899 174340 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551058 174340 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 526 11 5 4 5.0 N=C(N)NCCC[C@H](NC(=O)c1cc(-c2ccccc2)c(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064018 209178 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
17753143 85940 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 85940 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
117634981 114968 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 114968 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
155526496 171134 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4458380 171134 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
17753143 85940 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 85940 4 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
101886252 114969 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 114969 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
155516924 170150 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL4444281 170150 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
117634981 114968 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 114968 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
155526496 171134 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4458380 171134 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 416 11 5 4 2.9 CCC(Cc1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
101886252 114969 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 114969 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
155516924 170150 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL4444281 170150 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 538 12 4 7 3.8 COC(=O)[C@H](CCCNC(=N)N)NC(=O)c1sc(C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1C 10.1021/acs.jmedchem.9b00927
CHEMBL2064011 209171 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155546129 173515 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4530755 173515 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL1170644 208574 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
155555271 174344 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551118 174344 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
155546129 173515 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4530755 173515 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 402 10 5 4 2.7 CCC(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
155555271 174344 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4551118 174344 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 504 10 5 4 4.3 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)c2c1CCCC2)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064019 209179 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
3529 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
5311120 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL389348 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilizationAntagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
101886251 114965 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 114965 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
155518058 170242 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4445758 170242 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155518058 170242 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4445758 170242 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 532 10 5 4 5.0 Cc1cc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155510486 174713 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559976 174713 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155557328 174642 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4558167 174642 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155536326 172151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4473192 172151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155557328 174642 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4558167 174642 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
44430514 150242 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL395233 150242 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
122392666 165837 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ releaseAntagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ release
ChEMBL 463 9 4 5 3.0 N=C(N)NCCC[C@@H](C(=O)O)N1Cc2nc(C(c3ccccc3)c3ccccc3)sc2C1=O 10.1021/acs.jmedchem.7b00882
CHEMBL4248716 165837 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ releaseAntagonist activity at C3aR in HMDM assessed as inhibition of agonist-induced Ca2+ release
ChEMBL 463 9 4 5 3.0 N=C(N)NCCC[C@@H](C(=O)O)N1Cc2nc(C(c3ccccc3)c3ccccc3)sc2C1=O 10.1021/acs.jmedchem.7b00882
155536326 172151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4473192 172151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.0 Cc1cc(C(c2ccc(F)cc2)c2ccc(F)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
155557799 174695 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559463 174695 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
101886253 114964 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 114964 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
101886251 114965 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 114965 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
3529 3517 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 3517 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 3517 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
155563876 175271 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4572633 175271 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
101886253 114964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 114964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155510486 174713 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559976 174713 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 456 10 5 4 3.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)C2CCCCC2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064017 209177 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155557799 174695 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4559463 174695 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccn2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155563876 175271 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL4572633 175271 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 414 9 5 4 3.0 CC(C)=C(c1ccccc1)c1ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s1 10.1021/acs.jmedchem.9b00927
CHEMBL2064014 209174 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
CHEMBL2063898 209170 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155569071 176159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4592883 176159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
155569071 176159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4592883 176159 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 528 10 5 4 4.1 N=C(N)NCCC[C@H](NC(=O)c1sc(C(c2ccccc2)c2ccccc2)cc1Br)C(=O)O 10.1021/acs.jmedchem.9b00927
118716617 114963 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 114963 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155527368 171240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4459830 171240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155527368 171240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4459830 171240 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 518 10 5 4 4.7 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155534696 171979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 171979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
89570464 169819 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4439578 169819 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155535658 172098 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472490 172098 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL2064020 209180 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
89570464 169819 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4439578 169819 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 451 10 5 5 2.8 N=C(N)NCCC[C@H](NC(=O)c1cnc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
44430510 159118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL409773 159118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAntagonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL1170028 208541 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
118716617 114963 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 114963 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
155535658 172098 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
CHEMBL4472490 172098 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 510 12 5 6 3.4 COc1ccc(C(c2ccc(OC)cc2)c2ccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)s2)cc1 10.1021/acs.jmedchem.9b00927
155534696 171979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 171979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064015 209175 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm201609k
25156014 175449 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 175449 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
155534229 171938 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470384 171938 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
8384 1113 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 1113 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 1113 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
155534229 171938 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470384 171938 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 496 10 7 6 3.1 Cc1cc(C(c2ccc(O)cc2)c2ccc(O)cc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
25156014 175449 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 175449 2 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL2064018 209178 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate readerAntagonist activity at C3a receptor in dbcAMP differentiated human U937 cells assessed as inhibition of increase in intracellular calcium compound preincubated for 10 mins using Fluo-R staining by microplate reader
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm201609k
CHEMBL2064016 209176 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assayAntagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm201609k
155525092 170940 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4455385 170940 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assayAntagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay
ChEMBL 500 10 5 4 4.5 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccc3ccccc3c2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
127035774 136437 0 None - 1 Human 6.9 pKd = 6.9 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 136437 0 None - 1 Human 6.9 pKd = 6.9 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of 3-Indole carboxylic acid-leucine-oxazole-arginine-OH-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
127035774 136437 0 None - 1 Human 6.8 pKd = 6.8 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 136437 0 None - 1 Human 6.8 pKd = 6.8 Functional
Antagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assayAntagonist activity against C3aR in human MDM cells assessed as inhibition of compound26-induced intracellular Ca2+ release measured for 60 secs by fluorescence assay
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
3640 769 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
In a calcium mobilisation assay using RBL-2H3 cells stably expressing the hC3aR.In a calcium mobilisation assay using RBL-2H3 cells stably expressing the hC3aR.
Guide to Pharmacology None None None None 9476119
3915 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1525 11 None - 1 Human 5.9 pEC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8380 267 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25446428
49799093 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5761 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1172879 1652 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
134813896 3659 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
60201789 3659 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
8379 3659 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22500977
5776 4129 0 None 8 2 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3640 769 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
8381 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
91827354 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
CHEMBL3342689 1029 3 None - 1 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 25259874
71566654 1005 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
9449 1005 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
CHEMBL3736108 1005 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 24257095
3915 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
3915 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3915 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
49799079 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
49799079 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
5760 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
5760 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
91933514 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
91933514 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
CHEMBL1170024 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2015217
CHEMBL1170024 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1525 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9476119
10595 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
145996525 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
CHEMBL4459627 2153 21 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.Inhibition of C3aR agonist-induced Ca2+ Release in human monocyte-derived macrophages.
Guide to Pharmacology 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 31910011
10224 805 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
10224 805 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
25254550 805 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26297549
25254550 805 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9145417
8384 1113 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
91827355 1113 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
CHEMBL3342676 1113 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 25259874
5777 1654 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
3529 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
3529 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
5311120 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
5311120 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
CHEMBL389348 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 11342658
CHEMBL389348 3517 9 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 33551801
3915 1525 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
49799079 1525 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
5760 1525 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
91933514 1525 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893
CHEMBL1170024 1525 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20527893


Get vendors


Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL1170042 208548 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
155534696 171979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 171979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
3915 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
49799079 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
5760 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
91933514 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
8381 1029 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
91827354 1029 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
CHEMBL3342689 1029 3 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 448 10 6 4 2.3 O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/jm500956p
3529 3517 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
5311120 3517 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL389348 3517 9 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
89570442 114972 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342686 114972 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
127035774 136437 0 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735614 136437 0 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells
ChEMBL 413 12 4 4 1.9 NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O 10.1016/j.bmcl.2015.10.038
118716617 114963 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 114963 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
101886251 114965 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342679 114965 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886252 114969 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 114969 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
44430549 151266 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396030 151266 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 487 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
117634981 114968 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 114968 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
44430552 88005 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234306 88005 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430556 88051 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 431 6 1 3 4.6 O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234523 88051 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 431 6 1 3 4.6 O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430526 144235 1 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL390464 144235 1 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 10.1016/j.bmcl.2007.04.023
44430559 88170 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 454 6 1 2 5.0 O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234730 88170 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 454 6 1 2 5.0 O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426471 85703 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228846 85703 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
117634952 136534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 136534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634952 136534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736505 136534 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 490 13 6 6 1.7 CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034743 136533 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
CHEMBL3736489 136533 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
127034743 136533 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
CHEMBL3736489 136533 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 542 15 6 6 3.3 CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 10.1016/j.bmcl.2015.10.038
89570392 136477 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 136477 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570392 136477 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736020 136477 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 512 12 6 6 2.4 CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570442 114972 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342686 114972 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 449 10 5 5 2.6 Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886252 114969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342683 114969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 511 11 5 5 4.0 N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O 10.1021/jm500956p
136110886 208002 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 389 6 1 2 4.5 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97303 208002 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 389 6 1 2 4.5 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
89570147 114970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342684 114970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
101886254 114966 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 114966 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL1170026 208539 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
101886254 114966 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
CHEMBL3342680 114966 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)no1)C(=O)O 10.1021/jm500956p
127036518 136375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 136375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127036518 136375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735048 136375 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 509 12 6 7 2.2 CC[C@H](C)[C@H](NC(=O)c1ccc2ccccc2n1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL1170029 208542 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
44430538 87725 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 Cc1cc(C)cc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL233671 87725 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 461 7 1 3 5.1 Cc1cc(C)cc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
44426458 86291 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 358 8 5 4 1.7 Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL231303 86291 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 358 8 5 4 1.7 Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
136110890 207519 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 411 7 1 3 4.9 COc1ccc2c(c1)/C(=N/CCc1ccc(C)cc1)N=C2NCCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94579 207519 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 411 7 1 3 4.9 COc1ccc2c(c1)/C(=N/CCc1ccc(C)cc1)N=C2NCCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
89570147 114970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
CHEMBL3342684 114970 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1nc(C(c2ccccc2)c2ccccc2)n(C)c1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm500956p
44430555 88050 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2ccc(F)nc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234522 88050 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2ccc(F)nc2)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430560 88171 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 448 6 1 2 5.3 O=C(NC1CCN(C(=O)/C=C/c2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234731 88171 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 448 6 1 2 5.3 O=C(NC1CCN(C(=O)/C=C/c2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430514 150242 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL395233 150242 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 427 7 1 3 4.0 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170026 208539 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
136110896 107724 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 390 6 1 3 3.9 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3cnccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL319113 107724 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 390 6 1 3 3.9 Fc1ccc(CC/N=C2\N=C(NCCc3ccc(F)cc3)c3cnccc32)cc1 10.1016/s0960-894x(01)00522-4
71566653 136430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 136430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566653 136430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735554 136430 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 548 14 6 6 3.2 CC[C@H](C)[C@H](NC(=O)C(c1ccccc1)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034744 136406 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
CHEMBL3735339 136406 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 468 11 6 7 2.0 Cc1oc([C@H](CC(C)C)NC(=O)OC(C)(C)C)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1016/j.bmcl.2015.10.038
3529 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
5311120 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL389348 3517 9 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/jm1003705
CHEMBL1170029 208542 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565581 136348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734765 136348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565581 136348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734765 136348 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 546 12 6 6 3.1 CC(C)C[C@H](NC(=O)C1c2ccccc2-c2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44426496 142042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387755 142042 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(Cl)c2)c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
101886253 114964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 114964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
71565580 136484 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 136484 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565506 136476 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 136476 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565506 136476 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735993 136476 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 511 13 7 6 2.0 CC[C@H](C)[C@H](NC(=O)Cc1c[nH]c2ccccc12)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170639 208570 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71565580 136484 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736125 136484 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 590 16 6 7 3.7 CC[C@H](C)[C@H](NC(=O)CCC(=O)c1ccc(-c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170639 208570 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71565509 136424 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735465 136424 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
101886253 114964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342678 114964 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 411 12 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)CNCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
71565509 136424 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735465 136424 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 562 14 6 7 2.9 CC[C@H](C)[C@H](NC(=O)c1ccc(C(=O)c2ccccc2)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
44430548 87956 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234101 87956 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(F)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426497 85735 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229006 85735 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 502 10 5 4 4.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1169838 208537 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430510 159118 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
CHEMBL409773 159118 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 509 5 1 4 5.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2cc(Cl)ccc2Oc2ccc(Cl)cc21 10.1016/j.bmcl.2007.04.023
44426466 142034 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 8 5 4 2.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL387686 142034 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 8 5 4 2.7 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2Cl)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430553 88049 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ncccc1CCC(=O)N1CCC(NC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL234521 88049 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ncccc1CCC(=O)N1CCC(NC(=O)C(c2ccccc2)C2CCCCC2)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL1169838 208537 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 208563 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170436 208563 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
135418443 107920 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 353 4 1 2 4.8 Cc1ccc(C/N=C2\N=C(NCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL319332 107920 3 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 353 4 1 2 4.8 Cc1ccc(C/N=C2\N=C(NCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
71566580 114971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342685 114971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
71768012 136452 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 136452 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566580 114971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342685 114971 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 435 10 5 5 2.3 N=C(N)NCCC[C@H](NC(=O)c1coc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44430541 87726 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 467 7 1 3 5.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL233675 87726 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 467 7 1 3 5.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44431783 87940 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 4 4.5 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccsc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234005 87940 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 7 1 4 4.5 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccsc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426462 86393 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 369 8 5 5 1.3 N#Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL231404 86393 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 369 8 5 5 1.3 N#Cc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44426464 96911 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 396 8 5 4 2.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccc(F)c(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL265866 96911 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 396 8 5 4 2.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccc(F)c(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426460 166330 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 10 5 5 1.8 CCOc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL427268 166330 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 10 5 5 1.8 CCOc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44430546 87955 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1Cl)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234100 87955 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1Cl)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
44430558 151506 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 450 7 1 2 5.2 O=C(NC1CCN(C(=O)CCc2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396262 151506 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 450 7 1 2 5.2 O=C(NC1CCN(C(=O)CCc2ccccc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430516 87005 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 495 7 1 3 5.3 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL232418 87005 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 495 7 1 3 5.3 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2007.04.023
155534696 171979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4470864 171979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 464 10 5 4 3.7 Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/acs.jmedchem.9b00927
3915 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
49799079 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
5760 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
91933514 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170024 1525 11 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71768012 136452 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735760 136452 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC(C)C[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 3517 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
5311120 3517 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL389348 3517 9 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cellsDisplacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.7b00882
CHEMBL1170042 208548 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170644 208574 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170644 208574 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O 10.1021/jm1003705
CHEMBL1170230 208557 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170230 208557 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170025 208538 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170025 208538 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430536 86754 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccccc1C(C(=O)NC1CCN(C(=O)CCc2cccnc2)CC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL232029 86754 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccccc1C(C(=O)NC1CCN(C(=O)CCc2cccnc2)CC1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430529 87327 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 7 1 3 4.8 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)/C(=C/C1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL233232 87327 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 7 1 3 4.8 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)/C(=C/C1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
71566652 136538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 136538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566652 136538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736519 136538 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 458 12 6 6 1.6 CC[C@H](C)[C@H](NC(=O)c1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170033 208545 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170046 208552 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170046 208552 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
71566581 136504 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 136504 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
25156014 175449 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 175449 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
71566581 136504 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736239 136504 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 454 11 6 7 1.7 CC[C@H](C)[C@H](NC(=O)OC(C)(C)C)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
101886250 114975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 114975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
101886250 114975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
CHEMBL3342690 114975 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 462 10 5 5 2.4 Cc1c(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)nc(C(c2ccccc2)c2ccccc2)n1C 10.1021/jm500956p
44430554 151269 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL396031 151269 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 451 7 1 3 4.6 O=C(NC1CCN(C(=O)CCc2cccnc2F)CC1)C(c1ccccc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426495 85734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL229005 85734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 470 10 5 4 3.2 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
11252 770 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 770 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 770 39 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430550 88003 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 478 8 1 5 4.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc([N+](=O)[O-])cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234304 88003 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 478 8 1 5 4.4 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc([N+](=O)[O-])cc1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44426469 85679 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 400 8 5 5 2.6 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2csc3ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228634 85679 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 400 8 5 5 2.6 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2csc3ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426457 142877 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 362 8 5 4 1.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL389349 142877 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 362 8 5 4 1.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(F)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426459 149373 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 5 5 1.4 COc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
CHEMBL394538 149373 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 5 5 1.4 COc1cccc(-c2ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o2)c1 10.1016/j.bmcl.2007.04.022
44430532 87329 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 417 7 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CC=CC1 10.1016/j.bmcl.2007.04.023
CHEMBL233234 87329 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 417 7 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CC=CC1 10.1016/j.bmcl.2007.04.023
CHEMBL1170033 208545 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110895 207792 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 410 5 2 3 4.8 CC(=O)Nc1ccc2c(c1)/C(=N\Cc1ccc(C)cc1)N=C2NCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL96138 207792 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 410 5 2 3 4.8 CC(=O)Nc1ccc2c(c1)/C(=N\Cc1ccc(C)cc1)N=C2NCc1ccc(C)cc1 10.1016/s0960-894x(01)00522-4
44426470 85680 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 8 5 5 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc3c2oc2ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228635 85680 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 8 5 5 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc3c2oc2ccccc23)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
25156014 175449 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL4576800 175449 2 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 450 10 5 4 3.4 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)s1)C(=O)O 10.1021/acs.jmedchem.9b00927
CHEMBL1170638 208569 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170638 208569 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
127034742 136467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735887 136467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
127034742 136467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735887 136467 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 617 14 6 7 3.3 CC(C)C[C@H](NC(=O)C(C)c1ccc(N2Cc3ccccc3C2=O)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
136110894 208023 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.2 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3cc(Cl)c(Cl)cc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97420 208023 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.2 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3cc(Cl)c(Cl)cc32)cc1 10.1016/s0960-894x(01)00522-4
71525749 136429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 136429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71525749 136429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735507 136429 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 537 12 6 7 1.8 CC[C@H](C)[C@H](NC(=O)c1cncc(Br)c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
24829327 165458 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assayDisplacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay
ChEMBL 463 9 5 5 1.1 N=C(N)NCCC[C@H](NC(=O)c1cccn(Cc2ccccc2Br)c1=O)C(=O)O 10.1021/acs.jmedchem.7b00882
CHEMBL4239466 165458 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assayDisplacement of 125I-C3a from recombinant human C3aR expressed in HEK293 cell membranes after 3 hrs by scintillation proximity assay
ChEMBL 463 9 5 5 1.1 N=C(N)NCCC[C@H](NC(=O)c1cccn(Cc2ccccc2Br)c1=O)C(=O)O 10.1021/acs.jmedchem.7b00882
17753143 85940 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 85940 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
101886249 114967 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 114967 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
44430547 168859 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL438129 168859 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 465 7 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cccc(Cl)c1)C1C=CCCC1 10.1016/j.bmcl.2007.04.023
3529 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
3529 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
5311120 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
CHEMBL389348 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2007.04.022
11252 770 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 770 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 770 39 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430557 88169 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 6 1 3 4.9 Cc1cncc(/C=C/C(=O)N2CCC(NC(=O)C(c3ccccc3)C3CCCCC3)CC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL234729 88169 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 445 6 1 3 4.9 Cc1cncc(/C=C/C(=O)N2CCC(NC(=O)C(c3ccccc3)C3CCCCC3)CC2)c1 10.1016/j.bmcl.2007.04.023
44426478 85717 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 452 9 5 4 1.8 N=C(N)NCCC[C@@H](NC(=O)N1CCN(C(c2ccccc2)c2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228900 85717 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 452 9 5 4 1.8 N=C(N)NCCC[C@@H](NC(=O)N1CCN(C(c2ccccc2)c2ccccc2)CC1)C(=O)O 10.1016/j.bmcl.2007.04.022
136110893 207515 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 476 10 1 4 4.5 CN(C)CCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94544 207515 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 476 10 1 4 4.5 CN(C)CCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
101886249 114967 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342681 114967 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1noc(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
71565510 136393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 136393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 136454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 136454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
3529 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
5311120 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
CHEMBL389348 3517 9 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 412 12 4 4 1.5 O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b00927
17753143 85940 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL230034 85940 4 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
71565510 136393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735240 136393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 566 14 6 7 3.3 CC[C@H](C)[C@H](NC(=O)C(C)c1ccc2cc(OC)ccc2c1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71565582 136454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735764 136454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 550 14 6 7 3.4 CC[C@H](C)[C@H](NC(=O)c1ccccc1Oc1ccccc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170030 208543 11 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110892 207965 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.7 CC(C/N=C1\N=C(NCC(C)c2ccc(Cl)cc2)c2ccccc21)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL97134 207965 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 449 6 1 2 6.7 CC(C/N=C1\N=C(NCC(C)c2ccc(Cl)cc2)c2ccccc21)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00522-4
136110887 207529 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 447 9 1 3 5.3 CCCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL94618 207529 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 447 9 1 3 5.3 CCCOc1ccc2c(c1)/C(=N/CCc1ccc(F)cc1)N=C2NCCc1ccc(F)cc1 10.1016/s0960-894x(01)00522-4
101886248 114974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 114974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
136110891 207369 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 381 6 1 2 4.9 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL93713 207369 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 381 6 1 2 4.9 Cc1ccc(CC/N=C2\N=C(NCCc3ccc(C)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
17753143 85940 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL230034 85940 4 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 434 10 5 4 2.9 N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430527 87254 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 469 7 1 3 4.7 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2007.04.023
CHEMBL233028 87254 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 469 7 1 3 4.7 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCC(F)(F)CC1 10.1016/j.bmcl.2007.04.023
44430539 87919 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL233879 87919 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 463 8 1 4 4.5 COc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL1170031 208544 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170030 208543 11 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170031 208544 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44426475 144669 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL390834 144669 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 394 8 5 4 2.5 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O 10.1016/j.bmcl.2007.04.022
44430528 87255 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 489 7 1 3 5.8 CC1(C)CC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC(C)(C)C1 10.1016/j.bmcl.2007.04.023
CHEMBL233029 87255 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 489 7 1 3 5.8 CC1(C)CC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC(C)(C)C1 10.1016/j.bmcl.2007.04.023
101886248 114974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
CHEMBL3342688 114974 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 434 10 6 4 2.0 N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O 10.1021/jm500956p
10595 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
8384 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
117634949 136450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735746 136450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634949 136450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3735746 136450 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1cccc(OC)c1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
136110889 106200 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1ccc(CC/N=C2\N=C(NCCc3ccc(Cl)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL313866 106200 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1ccc(CC/N=C2\N=C(NCCc3ccc(Cl)cc3)c3ccccc32)cc1 10.1016/s0960-894x(01)00522-4
CHEMBL1170027 208540 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
136110897 208009 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1cccc(CC/N=C2\N=C(NCCc3cccc(Cl)c3)c3ccccc32)c1 10.1016/s0960-894x(01)00522-4
CHEMBL97335 208009 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 421 6 1 2 5.6 Clc1cccc(CC/N=C2\N=C(NCCc3cccc(Cl)c3)c3ccccc32)c1 10.1016/s0960-894x(01)00522-4
117634979 136355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 136355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117634979 136355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3734832 136355 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 502 13 6 6 2.5 CC[C@H](C)[C@H](NC(=O)C1(C(C)C)C=CCC=C1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
89570463 114973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342687 114973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
17753265 86755 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1cccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
CHEMBL232031 86755 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1cccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2007.04.023
44426463 86394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL231405 86394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 378 8 5 4 2.0 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170027 208540 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm1003705
71565508 136496 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736195 136496 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
11252 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430519 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
CHEMBL390036 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 10.1016/j.bmcl.2007.04.023
44430530 87328 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 8 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(CC1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
CHEMBL233233 87328 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 8 1 3 4.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(CC1CCCCC1)c1ccccc1 10.1016/j.bmcl.2007.04.023
44430551 88004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL234305 88004 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 483 7 1 3 5.6 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 10.1016/j.bmcl.2007.04.023
44430533 142100 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
CHEMBL388204 142100 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 447 7 1 3 4.8 Cc1ccc(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)C2CCCCC2)cc1 10.1016/j.bmcl.2007.04.023
44430531 152593 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 419 7 1 3 4.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.04.023
CHEMBL397190 152593 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 419 7 1 3 4.1 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccccc1)C1CCCC1 10.1016/j.bmcl.2007.04.023
44426465 85672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 392 8 5 4 2.4 Cc1ccc(Cl)cc1-c1ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o1 10.1016/j.bmcl.2007.04.022
CHEMBL228582 85672 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 392 8 5 4 2.4 Cc1ccc(Cl)cc1-c1ccc(C(=O)N[C@H](CCCNC(=N)N)C(=O)O)o1 10.1016/j.bmcl.2007.04.022
44426472 85704 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228847 85704 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 388 8 5 3 2.5 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2cccc(Cl)c2)c1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426481 85718 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 444 10 5 3 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL228901 85718 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 444 10 5 3 3.3 N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)cc1)C(=O)O 10.1016/j.bmcl.2007.04.022
44426461 149375 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 6 5 0.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(CO)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL394539 149375 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay
ChEMBL 374 9 6 5 0.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(CO)c2)o1)C(=O)O 10.1016/j.bmcl.2007.04.022
CHEMBL1170646 208575 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
44430513 92362 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 5 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2007.04.023
CHEMBL243048 92362 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin
ChEMBL 439 5 1 3 3.9 O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C1c2ccccc2Cc2ccccc21 10.1016/j.bmcl.2007.04.023
10595 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
145996525 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
CHEMBL4459627 2153 21 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
ChEMBL 532 10 5 4 5.0 O=C(c1sc(cc1C)C(c1ccc(cc1)Cl)c1ccc(cc1)Cl)N[C@H](C(=O)O)CCCNC(=N)N 10.1021/acs.jmedchem.9b00927
8384 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
91827355 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
CHEMBL3342676 1113 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 428 12 5 4 2.4 NC(=N)NCCC[C@@H](C(=O)O)NC(=O)CSCC(c1ccccc1)c1ccccc1 10.1021/jm500956p
71565508 136496 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736195 136496 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 501 13 6 7 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(N(C)C)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL1170637 208568 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170637 208568 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
CHEMBL1170646 208575 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting
ChEMBL None None None None 10.1021/jm1003705
136110888 207860 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 325 4 1 2 4.1 CC(C)NC1=N/C(=N\CCc2ccc(Cl)cc2)c2ccccc21 10.1016/s0960-894x(01)00522-4
CHEMBL96477 207860 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assayInhibition of complement component 3a (C3a) binding to C3a receptor in human neutrophil based assay
ChEMBL 325 4 1 2 4.1 CC(C)NC1=N/C(=N\CCc2ccc(Cl)cc2)c2ccccc21 10.1016/s0960-894x(01)00522-4
89570463 114973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342687 114973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 510 11 6 4 3.7 N=C(N)NCCC[C@H](NC(=O)c1nc(C(c2ccccc2)c2ccccc2)[nH]c1-c1ccccc1)C(=O)O 10.1021/jm500956p
117637102 136530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 136530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
117637102 136530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
CHEMBL3736447 136530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 518 14 6 8 1.7 CC[C@H](C)[C@H](NC(=O)c1ccc(OC)cc1OC)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 10.1016/j.bmcl.2015.10.038
71566654 1005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 1005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 1005 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
71566654 1005 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
9449 1005 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
CHEMBL3736108 1005 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis
ChEMBL 497 12 6 6 1.9 CC(C[C@@H](c1occ(n1)C(=O)N[C@H](C(=O)O)CCCN=C(N)N)NC(=O)c1c[nH]c2c1cccc2)C 10.1016/j.bmcl.2015.10.038
118716617 114963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
CHEMBL3342677 114963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 410 12 5 3 2.8 N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O 10.1021/jm500956p
117634981 114968 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
CHEMBL3342682 114968 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method
ChEMBL 436 10 5 6 1.7 N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O 10.1021/jm500956p
11252 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
44430519 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
CHEMBL390036 770 39 None - 0 Human 6.1 pIC50 = 6.1 Binding
IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.IC50 determined in a radioligand displacement assay; displacing [<sup>125</sup>I]C3a from hC3a receptor expressed in HMC1 cells co-expressing aequorin.
Guide to Pharmacology 433 7 1 3 4.5 O=C(N1CCC(CC1)NC(=O)C(c1ccccc1)C1CCCCC1)CCc1cccnc1 17459702
11286 1597 0 None - 1 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28562031