Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
12455 3050 54 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
65080 3050 54 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
CHEMBL4105357 3050 54 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
12455 3050 54 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
65080 3050 54 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
CHEMBL4105357 3050 54 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assayActivation of full-length human TAS2R16 expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio in presence of (E)-4-(2,2,3-trimethylcyclopent-3-enyl)but-2-enoic acid by Fluo-4 dye based FLIPR assay
ChEMBL 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O nan
1499 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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 2060 43 None -63 36 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R16 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
12451 1287 0 None - 1 Human 1.7 pEC50 = 1.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 457 7 7 12 -3.1 C1=CC=C(C=C1)C(C#N)OC2C(C(C(C(O2)COC3C(C(C(C(O3)CO)O)O)O)O)O)O 12379855
2180 1287 0 None - 1 Human 1.7 pEC50 = 1.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 457 7 7 12 -3.1 C1=CC=C(C=C1)C(C#N)OC2C(C(C(C(O2)COC3C(C(C(C(O3)CO)O)O)O)O)O)O 12379855
CHEMBL1967951 1287 0 None - 1 Human 1.7 pEC50 = 1.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 457 7 7 12 -3.1 C1=CC=C(C=C1)C(C#N)OC2C(C(C(C(O2)COC3C(C(C(C(O3)CO)O)O)O)O)O)O 12379855
12452 608 0 None - 1 Human 2.4 pEC50 = 2.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 4 8 11 -5.4 C([C@@H]1[C@H]([C@@H]([C@H]([C@@H](O1)OC[C@@H]2[C@H]([C@@H]([C@H]([C@@H](O2)O)O)O)O)O)O)O)O 20965151
441422 608 0 None - 1 Human 2.4 pEC50 = 2.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 4 8 11 -5.4 C([C@@H]1[C@H]([C@@H]([C@H]([C@@H](O1)OC[C@@H]2[C@H]([C@@H]([C@H]([C@@H](O2)O)O)O)O)O)O)O)O 20965151
CHEMBL1360334 608 0 None - 1 Human 2.4 pEC50 = 2.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 342 4 8 11 -5.4 C([C@@H]1[C@H]([C@@H]([C@H]([C@@H](O1)OC[C@@H]2[C@H]([C@@H]([C@H]([C@@H](O2)O)O)O)O)O)O)O)O 20965151
12454 3406 0 None - 1 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 4 5 7 -1.6 C1=CC=C(C(=C1)CO)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O 12379855
439503 3406 0 None - 1 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 286 4 5 7 -1.6 C1=CC=C(C(=C1)CO)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O 12379855
12455 3050 54 None - 1 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O 12379855
65080 3050 54 None - 1 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O 12379855
CHEMBL4105357 3050 54 None - 1 Human 3.0 pEC50 = 3.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 256 3 4 6 -1.1 C1=CC=C(C=C1)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O 12379855
12453 123 0 None - 1 Human 3.2 pEC50 = 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 301 4 4 8 -1.2 OC[C@H]1O[C@@H](OC2=CC=C(C=C2)[N+]([O-])=O)[C@@H](O)[C@@H](O)[C@@H]1O 28798468
161880 123 0 None - 1 Human 3.2 pEC50 = 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 301 4 4 8 -1.2 OC[C@H]1O[C@@H](OC2=CC=C(C=C2)[N+]([O-])=O)[C@@H](O)[C@@H](O)[C@@H]1O 28798468
CHEMBL4462691 123 0 None - 1 Human 3.2 pEC50 = 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 301 4 4 8 -1.2 OC[C@H]1O[C@@H](OC2=CC=C(C=C2)[N+]([O-])=O)[C@@H](O)[C@@H](O)[C@@H]1O 28798468
2268 3121 0 None -1 2 Human 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
4357 3121 0 None -1 2 Human 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
4911 3121 0 None -1 2 Human 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
CHEMBL897 3121 0 None -1 2 Human 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
DB01032 3121 0 None -1 2 Human 3.5 pIC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI