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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
CHEMBL1170012 | 10602 | None | 37 | Human | Binding | EC50 | = | 29512.09 | 4.53 | - | 2 | Agonist activity at human FFA4 receptor expressed in CHO-K1 cells assessed as increase in amplitude of dynamic mass redistribution response by DMR assay | ChEMBL | 315.1 | 3 | 1 | 2 | 3.81 | Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2020.127650 | |
CHEMBL2315528 | 86563 | None | 0 | Human | Binding | EC50 | = | 4786.30 | 5.32 | - | 3 | Agonist activity at GPR120 (unknown origin) | ChEMBL | 289.1 | 4 | 1 | 2 | 3.17 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | https://dx.doi.org/10.1021/jm301470a | |
CHEMBL2315528 | 86563 | None | 0 | Human | Binding | EC50 | = | 776.25 | 6.11 | - | 3 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 289.1 | 4 | 1 | 2 | 3.17 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386354 | 90395 | None | 0 | Human | Binding | EC50 | = | 3890.45 | 5.41 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 307.1 | 4 | 1 | 2 | 3.31 | N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386355 | 90396 | None | 0 | Human | Binding | EC50 | = | 1380.38 | 5.86 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 321.1 | 5 | 1 | 2 | 3.70 | N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386357 | 90398 | None | 0 | Human | Binding | EC50 | = | 91201.08 | 4.04 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 251.1 | 3 | 1 | 2 | 2.50 | O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386358 | 90399 | None | 0 | Human | Binding | EC50 | = | 5754.40 | 5.24 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 268.1 | 3 | 1 | 1 | 3.24 | O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386359 | 90400 | None | 0 | Human | Binding | EC50 | = | 7943.28 | 5.10 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 268.1 | 3 | 1 | 1 | 3.24 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386360 | 90401 | None | 0 | Human | Binding | EC50 | = | 8317.64 | 5.08 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 286.1 | 3 | 1 | 1 | 3.38 | O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386361 | 90402 | None | 0 | Human | Binding | EC50 | = | 1584.89 | 5.80 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 282.1 | 3 | 1 | 1 | 3.55 | Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386362 | 90403 | None | 0 | Human | Binding | EC50 | = | 3890.45 | 5.41 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 282.1 | 3 | 1 | 1 | 3.55 | Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386363 | 90404 | None | 0 | Human | Binding | EC50 | = | 9549.93 | 5.02 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 307.1 | 3 | 1 | 2 | 3.42 | Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386364 | 90405 | None | 0 | Human | Binding | EC50 | = | 1174.90 | 5.93 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 336.1 | 4 | 1 | 1 | 4.32 | O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386365 | 90406 | None | 0 | Human | Binding | EC50 | = | 3162.28 | 5.50 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 336.0 | 3 | 1 | 1 | 4.55 | O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386367 | 90408 | None | 0 | Human | Binding | EC50 | = | 64565.42 | 4.19 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 360.1 | 5 | 1 | 3 | 2.79 | CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386368 | 90409 | None | 0 | Human | Binding | EC50 | = | 300.00 | 6.52 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 404.1 | 8 | 1 | 4 | 2.80 | CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386369 | 90410 | None | 0 | Human | Binding | EC50 | = | 300.00 | 6.52 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 404.1 | 8 | 1 | 4 | 2.80 | CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386370 | 90412 | None | 0 | Human | Binding | EC50 | = | 300.00 | 6.52 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 418.1 | 9 | 1 | 4 | 3.19 | CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL2386371 | 90413 | None | 0 | Human | Binding | EC50 | = | 300.00 | 6.52 | - | 2 | Agonist activity at C-terminal yellow fluorescent protein-fused human FFA4 receptor transfected in HEK293 cells after 5 mins by BRET assay | ChEMBL | 418.1 | 9 | 1 | 4 | 3.19 | CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/ml4000673 | |
CHEMBL3311302 | 113086 | None | 38 | Human | Binding | IC50 | = | 79.43 | 7.10 | - | 3 | Inhibition of human FFA4 receptor expressed in U2OS cells | ChEMBL | 351.1 | 3 | 1 | 3 | 4.17 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | https://dx.doi.org/10.1016/j.bmcl.2014.05.012 |
Showing 1 to 20 of 274 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
α-linolenic acid | 363 | None | 48 | Human | Functional | pEC50 | = | - | 5.50 | -1 | 3 | Unclassified | Guide to Pharmacology | 278.2 | 13 | 1 | 1 | 5.66 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/22519963 | |
α-linolenic acid | 363 | None | 48 | Human | Functional | EC50 | = | 3235.94 | 5.49 | -1 | 3 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 278.2 | 13 | 1 | 1 | 5.66 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | https://dx.doi.org/10.1021/jm300215x | |
α-linolenic acid | 363 | None | 48 | Human | Functional | EC50 | = | 2600.00 | 5.58 | -1 | 3 | Agonist activity at human GPR120-G-alpha-16 fusion protein expressed in Flp-in HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay | ChEMBL | 278.2 | 13 | 1 | 1 | 5.66 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | https://dx.doi.org/10.1021/jm800970b | |
α-linolenic acid | 363 | None | 48 | Rat | Functional | pEC50 | = | - | 5.06 | -4 | 3 | Unclassified | Guide to Pharmacology | 278.2 | 13 | 1 | 1 | 5.66 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/18320172 | |
BAY 60-6583 | 585 | None | 42 | Human | Functional | EC50 | = | 1178.07 | 5.93 | -38 | 8 | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | ChEMBL | 379.1 | 7 | 2 | 7 | 2.44 | N#Cc1c(N)nc(SCC(N)=O)c(C#N)c1-c1ccc(OCC2CC2)cc1 | https://dx.doi.org/10.6019/CHEMBL5442687 | |
BENZYLOXYPHENYLPROPANOIC ACID | 58844 | None | 46 | Human | Functional | EC50 | = | 11748.98 | 4.93 | -20 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 256.1 | 6 | 1 | 2 | 3.28 | O=C(O)CCc1ccc(OCc2ccccc2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
BP 897 | 708 | None | 33 | Human | Functional | EC50 | = | 1479.66 | 5.83 | -2754 | 31 | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | ChEMBL | 417.2 | 8 | 1 | 4 | 4.18 | COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3c2)CC1 | https://dx.doi.org/10.6019/CHEMBL5442687 | |
CHEMBL1581959 | 51435 | None | 11 | Human | Functional | EC50 | = | 794.33 | 6.10 | - | 1 | Agonist activity at human FFA4 receptor expressed in U2OS cells assessed as calcium mobilization after 24 hrs by FLIPR | ChEMBL | 339.1 | 4 | 1 | 3 | 4.08 | COc1cc(S(=O)(=O)Nc2c(C)cc(C)cc2C)ccc1Cl | https://dx.doi.org/10.1016/j.bmcl.2014.05.012 | |
CHEMBL1688454 | 58846 | None | 0 | Human | Functional | EC50 | = | 16595.87 | 4.78 | -77 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 348.1 | 8 | 1 | 3 | 5.08 | O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1688455 | 58847 | None | 2 | Human | Functional | EC50 | = | 371.54 | 6.43 | 15 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 332.1 | 7 | 1 | 2 | 4.95 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1688455 | 58847 | None | 2 | Human | Functional | EC50 | = | 396.20 | 6.40 | 15 | 2 | Agonist activity at human FFAR4 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by luminescence assay | ChEMBL | 332.1 | 7 | 1 | 2 | 4.95 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | https://dx.doi.org/10.1016/j.bmc.2017.10.040 | |
CHEMBL1688457 | 58849 | None | 0 | Human | Functional | EC50 | = | 2398.83 | 5.62 | -11 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 332.1 | 7 | 1 | 2 | 4.95 | O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1688458 | 58850 | None | 0 | Human | Functional | EC50 | = | 562.34 | 6.25 | -14 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 348.1 | 8 | 1 | 3 | 5.08 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1688458 | 58850 | None | 0 | Human | Functional | EC50 | = | 968.00 | 6.01 | -14 | 2 | Agonist activity at human FFA4 receptor expressed in human U2OS cells co-expressing Galpha16 assessed as calcium mobilization by Fluo-4 dye based FLIPR assay | ChEMBL | 348.1 | 8 | 1 | 3 | 5.08 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2017.01.034 | |
CHEMBL1688465 | 58858 | None | 0 | Human | Functional | EC50 | = | 8709.64 | 5.06 | -107 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 346.2 | 7 | 1 | 2 | 5.26 | Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1688473 | 58866 | None | 0 | Human | Functional | EC50 | = | 8317.64 | 5.08 | -660 | 3 | Agonist activity at GPR120 assessed as stimulation of calcium mobilization | ChEMBL | 378.2 | 7 | 1 | 2 | 5.71 | Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 | https://dx.doi.org/10.1021/jm3002026 | |
CHEMBL1773252 | 61823 | None | 2 | Human | Functional | EC50 | = | 5370.32 | 5.27 | -17 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 334.0 | 6 | 1 | 2 | 4.04 | O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1773253 | 61824 | None | 0 | Human | Functional | EC50 | = | 1737.80 | 5.76 | -3 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 334.0 | 6 | 1 | 2 | 4.04 | O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1773254 | 61825 | None | 2 | Human | Functional | EC50 | = | 478.63 | 6.32 | -5 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 334.0 | 6 | 1 | 2 | 4.04 | O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 | https://dx.doi.org/10.1021/jm300215x | |
CHEMBL1773255 | 61826 | None | 0 | Human | Functional | EC50 | = | 20892.96 | 4.68 | -33 | 2 | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | ChEMBL | 281.1 | 6 | 1 | 3 | 3.15 | N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 | https://dx.doi.org/10.1021/jm300215x |
Showing 1 to 20 of 477 entries