Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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
102331684 114741 0 None - 1 Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D after 30 mins by inositol phosphate turnover assayAgonist activity at mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D after 30 mins by inositol phosphate turnover assay
ChEMBL 186 4 5 3 -1.3 N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O 10.1039/C1MD00186H
CHEMBL3347673 114741 0 None - 1 Mouse 4.1 pEC50 = 4.1 Functional
Agonist activity at mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D after 30 mins by inositol phosphate turnover assayAgonist activity at mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D after 30 mins by inositol phosphate turnover assay
ChEMBL 186 4 5 3 -1.3 N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O 10.1039/C1MD00186H
8693156 123576 1 None - 1 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633655 123576 1 None - 1 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
8693156 123576 1 None - 1 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633655 123576 1 None - 1 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
9044803 123573 9 None 1 2 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 123573 9 None 1 2 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
9044803 123573 9 None 1 2 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633650 123573 9 None 1 2 Mouse 4.7 pIC50 = 4.7 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 391 6 1 4 2.8 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
122195442 123574 0 None - 1 Mouse 4.4 pIC50 = 4.4 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633651 123574 0 None - 1 Mouse 4.4 pIC50 = 4.4 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
122195442 123574 0 None - 1 Mouse 4.4 pIC50 = 4.4 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633651 123574 0 None - 1 Mouse 4.4 pIC50 = 4.4 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 409 6 1 4 2.9 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 10.1021/acs.jmedchem.5b01254
122195453 123578 0 None 2 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 123578 0 None 2 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195453 123578 0 None 2 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633663 123578 0 None 2 2 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 431 5 1 4 3.6 O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
17521846 123579 5 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 375 6 1 3 3.6 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633664 123579 5 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 375 6 1 3 3.6 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 10.1021/acs.jmedchem.5b01254
17521846 123579 5 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 375 6 1 3 3.6 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 10.1021/acs.jmedchem.5b01254
CHEMBL3633664 123579 5 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 375 6 1 3 3.6 CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 10.1021/acs.jmedchem.5b01254
122195454 123580 0 None 8 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 123580 0 None 8 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195454 123580 0 None 8 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
CHEMBL3633665 123580 0 None 8 2 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 377 7 1 4 3.3 CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 10.1021/acs.jmedchem.5b01254
122195445 123575 0 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 10.1021/acs.jmedchem.5b01254
CHEMBL3633654 123575 0 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 10.1021/acs.jmedchem.5b01254
122195445 123575 0 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 10.1021/acs.jmedchem.5b01254
CHEMBL3633654 123575 0 None - 1 Mouse 4.2 pIC50 = 4.2 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 10.1021/acs.jmedchem.5b01254
122195446 123577 0 None 1 5 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 123577 0 None 1 5 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
122195446 123577 0 None 1 5 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
CHEMBL3633656 123577 0 None 1 5 Mouse 5.0 pIC50 = 5.0 Functional
Antagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assayAntagonist activity at mouse GPRC6A receptor expressed in HEK293 cells assessed as inhibition of L-ornithine-induced inositol monophosphate accumulation after 1 hr by FRET assay
ChEMBL 421 7 1 5 2.8 COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 10.1021/acs.jmedchem.5b01254
3401 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
6262 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
725 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
88747248 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
CHEMBL446143 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
DB00129 2304 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN None
1549 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
28782 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
6322 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
721 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
CHEMBL1485 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
DB00125 2238 106 None -1 3 Human 8.4 pEC50 = 8.4 Functional
NoneNone
Drug Central 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N None
1311 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
4633 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
4634 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
5961 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
6992086 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
723 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
CHEMBL930 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
DB00130 2277 0 None - 1 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 4 3 3 -1.3 NC(=O)CC[C@@H](C(=O)O)N 15576628
4127 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
5951 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
6857581 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
726 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
CHEMBL11298 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
DB00133 2318 113 None -1348 2 Human 3.2 pEC50 None 3.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 105 2 3 3 -1.6 OC[C@@H](C(=O)O)N 15576628
1319 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
4084 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
4635 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
5257127 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
727 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
750 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
CHEMBL773 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
DB00145 1788 123 None -12302 2 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 75 1 2 2 -1.0 NCC(=O)O 15576628
3103 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
6992098 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
722 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
9750 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
CHEMBL444814 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
DB00155 2249 0 None - 1 Human 3.6 pEC50 None 3.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 175 5 4 3 -1.2 NC(=O)NCCC[C@@H](C(=O)O)N 15576628
4255 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
4542 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
4543 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
5950 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
720 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
7311724 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
CHEMBL279597 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
DB00160 2230 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 89 1 2 2 -0.6 C[C@@H](C(=O)O)N 15576628
122198194 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
1622 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
5962 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
71774817 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
724 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
CHEMBL8085 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
DB00123 2296 0 None - 1 Human 3.8 pEC50 None 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 146 5 3 3 -0.5 NCCCC[C@@H](C(=O)O)N 15576628
3401 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
6262 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
725 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
88747248 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
CHEMBL446143 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
DB00129 2304 0 None - 1 Human 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 132 4 3 3 -0.9 N[C@H](C(=O)O)CCCN 15576628
1549 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
28782 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
6322 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
721 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
CHEMBL1485 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
DB00125 2238 106 None -1 3 Human 4.4 pEC50 None 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 174 5 4 3 -1.5 OC(=O)[C@H](CCCN=C(N)N)N 15576628
719 770 2 None -27 3 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 19836834
9882793 770 2 None -27 3 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 19836834
CHEMBL1801356 770 2 None -27 3 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 300 4 2 1 5.2 C[C@H](c1cccc2c1cccc2)NCc1cc2c([nH]1)cccc2 19836834
6918446 2823 52 None -616 6 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 19836834
716 2823 52 None -616 6 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 19836834
CHEMBL180672 2823 52 None -616 6 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 19836834
DB05695 2823 52 None -616 6 Mouse 5.0 pIC50 ~ 5 Functional
This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).This is an inferred IC50 based on 10µM of the compound inhibiting maximum L-ornithine-induced activation of GPCR6 by approximately 50% (see Fig 1B in reference).
Guide to Pharmacology 408 8 2 4 4.7 N#Cc1c(cccc1Cl)OC[C@@H](CNC(Cc1ccc2c(c1)cccc2)(C)C)O 19836834


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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
102331684 114741 0 None - 1 Mouse 4.1 pKi = 4.1 Binding
Binding affinity to mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66DBinding affinity to mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D
ChEMBL 186 4 5 3 -1.3 N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O 10.1039/C1MD00186H
CHEMBL3347673 114741 0 None - 1 Mouse 4.1 pKi = 4.1 Binding
Binding affinity to mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66DBinding affinity to mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D
ChEMBL 186 4 5 3 -1.3 N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O 10.1039/C1MD00186H