Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb
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ligand
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selectivity
# Tested
GPCRs
Species

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

Assay
Description
Source

Mol
weight
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DOI

68344426 175696 0 None -4 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assay
ChEMBL 250 0 1 3 2.6 C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)C2CC1 nan
CHEMBL4582048 175696 0 None -4 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assay
ChEMBL 250 0 1 3 2.6 C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)C2CC1 nan
23259348 169913 0 None -3 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 250 0 1 3 2.6 C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 nan
CHEMBL4440983 169913 0 None -3 3 Human 4.5 pEC50 = 4.5 Functional
Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assay
ChEMBL 250 0 1 3 2.6 C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1 nan
1499 2091 47 None -63 38 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
3779 2091 47 None -63 38 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
536 2091 47 None -63 38 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
CHEMBL434 2091 47 None -63 38 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
DB01064 2091 47 None -63 38 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C nan
1499 2091 47 None -63 38 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 2091 47 None -63 38 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 2091 47 None -63 38 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 2091 47 None -63 38 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 2091 47 None -63 38 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
12460 253 0 None 1 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
36573 253 0 None 1 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
CHEMBL176687 253 0 None 1 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
5143 3457 0 None 1 2 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
5432 3457 0 None 1 2 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
CHEMBL310671 3457 0 None 1 2 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
12438 471 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 3 1 6 3.3 COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O 15537898
2236 471 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 3 1 6 3.3 COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O 15537898
CHEMBL93353 471 0 None -5 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 341 3 1 6 3.3 COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O 15537898
12470 1276 0 None -3 2 Human 1.8 pIC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
7533 1276 0 None -3 2 Human 1.8 pIC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
CHEMBL1206440 1276 0 None -3 2 Human 1.8 pIC50 = 1.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
412 3460 46 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
73571 3460 46 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
CHEMBL448297 3460 46 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
DB08517 3460 46 None - 1 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
25099817 1802 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 198 4 1 1 3.3 CC1CCC(C1(C)C)CCCC(=O)O 20537538
9112 1802 0 None 1 3 Human 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 198 4 1 1 3.3 CC1CCC(C1(C)C)CCCC(=O)O 20537538




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

5379096 186407 93 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 330 3 3 7 2.6 COc1cc(-c2cc(=O)c3c(O)c(OC)c(O)cc3o2)ccc1O 10.1021/np200391c
CHEMBL487601 186407 93 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 330 3 3 7 2.6 COc1cc(-c2cc(=O)c3c(O)c(OC)c(O)cc3o2)ccc1O 10.1021/np200391c
44576022 186942 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 372 4 2 7 3.4 COc1cc([C@@H]2CC(=O)c3c(O)cc(O)cc3O2)ccc1OC(=O)C(C)C 10.1021/np200391c
CHEMBL490162 186942 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 372 4 2 7 3.4 COc1cc([C@@H]2CC(=O)c3c(O)cc(O)cc3O2)ccc1OC(=O)C(C)C 10.1021/np200391c
44412004 78261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 316 3 2 6 2.8 COc1cc2c(c(O)c1OC)C(=O)C[C@@H](c1ccc(O)cc1)O2 10.1021/np200391c
CHEMBL210692 78261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 316 3 2 6 2.8 COc1cc2c(c(O)c1OC)C(=O)C[C@@H](c1ccc(O)cc1)O2 10.1021/np200391c
412 3460 46 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 10.1021/np200391c
73571 3460 46 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 10.1021/np200391c
CHEMBL448297 3460 46 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 10.1021/np200391c
DB08517 3460 46 None - 3 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit
ChEMBL 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 10.1021/np200391c
13858192 113309 17 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assayAntagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assay
ChEMBL 362 5 1 3 5.1 C=C1CC[C@H]2C(C)(C)[C@@H](OC(C)=O)CC[C@]2(C)[C@H]1CC/C(C)=C/C(=O)O 10.1021/np5001413
CHEMBL3315351 113309 17 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assayAntagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assay
ChEMBL 362 5 1 3 5.1 C=C1CC[C@H]2C(C)(C)[C@@H](OC(C)=O)CC[C@]2(C)[C@H]1CC/C(C)=C/C(=O)O 10.1021/np5001413