Ligand source activities (1 row/activity)





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

68344426 175800 None 0 Human Functional pEC50 = 4.5 4.5 -4 3
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 175800 None 0 Human Functional pEC50 = 4.5 4.5 -4 3
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 170016 None 0 Human Functional pEC50 = 4.5 4.5 -3 3
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 170016 None 0 Human Functional pEC50 = 4.5 4.5 -3 3
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 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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
3779.0 2091 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
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 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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
3779.0 2091 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
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 None 0 Human Functional pEC50 = 2.6 2.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
36573 253 None 0 Human Functional pEC50 = 2.6 2.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
CHEMBL176687 253 None 0 Human Functional pEC50 = 2.6 2.6 1 2
UnclassifiedUnclassified
Guide to Pharmacology 163 0 1 4 -0.7 CC1=CC(=O)NS(=O)(=O)O1 15537898
5143 3457 None 0 Human Functional pEC50 = 3.0 3.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
5432 3457 None 0 Human Functional pEC50 = 3.0 3.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
CHEMBL310671 3457 None 0 Human Functional pEC50 = 3.0 3.0 1 2
UnclassifiedUnclassified
Guide to Pharmacology 183 0 1 3 0.1 O=C1NS(=O)(=O)c2c1cccc2 15537898
12438 471 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
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 None 0 Human Functional pIC50 = 1.8 1.8 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
7533 1276 None 0 Human Functional pIC50 = 1.8 1.8 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
CHEMBL1206440 1276 None 0 Human Functional pIC50 = 1.8 1.8 -3 2
UnclassifiedUnclassified
Guide to Pharmacology 179 2 2 2 0.7 C1CCC(CC1)NS(=O)(=O)O 28919036
412 3460 None 34 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
73571 3460 None 34 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
CHEMBL448297 3460 None 34 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
DB08517 3460 None 34 Human Functional pIC50 = 5.3 5.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 286 2 2 5 2.8 COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O 22059530
25099817 1802 None 0 Human Functional pIC50 = 5.5 5.5 1 3
UnclassifiedUnclassified
Guide to Pharmacology 198 4 1 1 3.3 CC1CCC(C1(C)C)CCCC(=O)O 20537538
9112 1802 None 0 Human Functional pIC50 = 5.5 5.5 1 3
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 Activity Chemical information
Sel. page 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

5379096 186513 None 55 Human Binding pIC50 = 5.0 5.0 - 0
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 186513 None 55 Human Binding pIC50 = 5.0 5.0 - 0
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 187048 None 1 Human Binding pIC50 = 5.7 5.7 - 0
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 187048 None 1 Human Binding pIC50 = 5.7 5.7 - 0
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 78290 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 78290 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 None 34 Human Binding pIC50 = 5.4 5.4 - 3
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 None 34 Human Binding pIC50 = 5.4 5.4 - 3
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 None 34 Human Binding pIC50 = 5.4 5.4 - 3
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 None 34 Human Binding pIC50 = 5.4 5.4 - 3
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 113372 None 15 Human Binding pIC50 = 5.1 5.1 - 0
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 113372 None 15 Human Binding pIC50 = 5.1 5.1 - 0
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
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