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
102331684 122031 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 122031 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 130886 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 130886 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 130886 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 130886 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 130883 11 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 130883 11 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 130883 11 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 130883 11 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 130884 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 130884 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 130884 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 130884 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 130888 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 130888 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 130888 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 130888 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 130889 4 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 130889 4 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 130889 4 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 130889 4 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 130890 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 130890 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 130890 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 130890 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 130885 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 130885 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 130885 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 130885 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 130887 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 130887 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 130887 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 130887 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 9125 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 9125 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 9125 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 9125 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 9125 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 9125 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 9096 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 9096 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 9096 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 9096 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 9096 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 9096 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 9096 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 9096 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 9139 117 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 9139 117 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 9139 117 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 9139 117 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 9139 117 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 9139 117 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 8607 130 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 8607 130 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 8607 130 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 8607 130 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 8607 130 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 8607 130 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 8607 130 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 8607 130 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 9071 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 9071 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 9071 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 9071 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 9071 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 9071 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 9050 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 9050 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 9050 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 9050 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 9050 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 9050 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 9050 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 9050 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 9117 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 9117 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 9117 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 9117 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 9117 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 9117 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 9117 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 9125 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 9125 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 9125 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 9125 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 9125 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 9125 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 9059 111 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 7571 5 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 7571 5 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 7571 5 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 9654 56 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 9654 56 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 9654 56 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 9654 56 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




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 122031 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 122031 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