Ligand source activities (1 row/activity)



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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

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 DOI
17725 15592 None 53 Human Functional pEC50 = 4 4.0 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 132 0 0 1 0.4 CN(C)C(=S)N(C)C nan
CHEMBL12214 15592 None 53 Human Functional pEC50 = 4 4.0 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 132 0 0 1 0.4 CN(C)C(=S)N(C)C nan
2723593 173351 None 36 Human Functional pEC50 = 4.8 4.8 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 118 0 2 2 -0.6 CC(=O)NC(N)=S nan
CHEMBL4524588 173351 None 36 Human Functional pEC50 = 4.8 4.8 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 118 0 2 2 -0.6 CC(=O)NC(N)=S nan
820777 136791 None 49 Human Functional pEC50 = 4.8 4.8 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 151 1 1 1 2.4 CC(=S)Nc1ccccc1 nan
CHEMBL3740596 136791 None 49 Human Functional pEC50 = 4.8 4.8 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 151 1 1 1 2.4 CC(=S)Nc1ccccc1 nan
12496 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N nan
676454 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N nan
CHEMBL263376 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N nan
DB03694 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N nan
2308 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 nan
657298 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 nan
6650 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 nan
CHEMBL1518 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 nan
DB00550 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 nan
700999 98422 None 55 Human Functional pEC50 = 5.6 5.6 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 228 2 2 1 3.5 S=C(Nc1ccccc1)Nc1ccccc1 nan
CHEMBL275260 98422 None 55 Human Functional pEC50 = 5.6 5.6 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 228 2 2 1 3.5 S=C(Nc1ccccc1)Nc1ccccc1 nan
1499 2091 None 34 Human Functional pEC50 = 8.3 8.3 -63 38
Agonist activity at human TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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
697057 15283 None 67 Human Functional pEC50 = 6.3 6.3 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 204 1 2 2 2.1 O=c1cc(-c2ccccc2)[nH]c(=S)[nH]1 nan
CHEMBL1212975 15283 None 67 Human Functional pEC50 = 6.3 6.3 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 204 1 2 2 2.1 O=c1cc(-c2ccccc2)[nH]c(=S)[nH]1 nan
69794 173622 None 47 Human Functional pEC50 = 4.3 4.3 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 89 1 0 1 0.5 CN(C)C=S nan
CHEMBL4530853 173622 None 47 Human Functional pEC50 = 4.3 4.3 - 1
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
ChEMBL 89 1 0 1 0.5 CN(C)C=S nan
2308 3188 None 68 Human Functional pEC50 = 8.2 8.2 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
Drug Central 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 None
657298 3188 None 68 Human Functional pEC50 = 8.2 8.2 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
Drug Central 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 None
6650 3188 None 68 Human Functional pEC50 = 8.2 8.2 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
Drug Central 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 None
CHEMBL1518 3188 None 68 Human Functional pEC50 = 8.2 8.2 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
Drug Central 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 None
DB00550 3188 None 68 Human Functional pEC50 = 8.2 8.2 34 2
Activity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assayActivity at human TAS2R38 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as effect on calcium response by FLIPR assay
Drug Central 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 None
1499 2091 None 34 Human Functional pEC50 = 8.1 8.1 -63 38
Agonist activity at human TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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 TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R38 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
1349907 2499 None 0 Human Functional pEC50 = 4.0 4.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 114 0 1 3 0.7 Cn1ccnc1S 23632915
1745 2499 None 0 Human Functional pEC50 = 4.0 4.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 114 0 1 3 0.7 Cn1ccnc1S 23632915
6649 2499 None 0 Human Functional pEC50 = 4.0 4.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 114 0 1 3 0.7 Cn1ccnc1S 23632915
CHEMBL1515 2499 None 0 Human Functional pEC50 = 4.0 4.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 114 0 1 3 0.7 Cn1ccnc1S 23632915
DB00763 2499 None 0 Human Functional pEC50 = 4.0 4.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 114 0 1 3 0.7 Cn1ccnc1S 23632915
12495 1834 None 0 Human Functional pEC50 = 4.2 4.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 129 1 1 2 0.4 C=CC1CNC(=S)O1 20551074
3034683 1834 None 0 Human Functional pEC50 = 4.2 4.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 129 1 1 2 0.4 C=CC1CNC(=S)O1 20551074
CHEMBL508652 1834 None 0 Human Functional pEC50 = 4.2 4.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 129 1 1 2 0.4 C=CC1CNC(=S)O1 20551074
12496 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N 15723792
676454 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N 15723792
CHEMBL263376 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N 15723792
DB03694 3101 None 59 Human Functional pEC50 = 5.7 5.7 2 2
UnclassifiedUnclassified
Guide to Pharmacology 152 1 2 1 1.3 C1=CC=C(C=C1)NC(=S)N 15723792
2308 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
UnclassifiedUnclassified
Guide to Pharmacology 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 15723792
657298 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
UnclassifiedUnclassified
Guide to Pharmacology 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 15723792
6650 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
UnclassifiedUnclassified
Guide to Pharmacology 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 15723792
CHEMBL1518 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
UnclassifiedUnclassified
Guide to Pharmacology 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 15723792
DB00550 3188 None 68 Human Functional pEC50 = 5.7 5.7 34 2
UnclassifiedUnclassified
Guide to Pharmacology 170 2 2 2 1.4 CCCc1cc(=O)[nH]c(=S)[nH]1 15723792
2268 3170 None 0 Human Functional pIC50 = 3.7 3.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
4357 3170 None 0 Human Functional pIC50 = 3.7 3.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
4911 3170 None 0 Human Functional pIC50 = 3.7 3.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
CHEMBL897 3170 None 0 Human Functional pIC50 = 3.7 3.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661
DB01032 3170 None 0 Human Functional pIC50 = 3.7 3.7 1 2
UnclassifiedUnclassified
Guide to Pharmacology 285 7 1 3 2.2 CCCN(S(=O)(=O)c1ccc(cc1)C(=O)O)CCC 21629661


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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