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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |
CHEMBL3347673 | 115317 | None | 0 | Mouse | Binding | Ki | = | 75857.76 | 4.12 | - | 1 | Binding affinity to mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D | ChEMBL | 186.1 | 4 | 5 | 3 | -1.34 | N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O | https://dx.doi.org/10.1039/C1MD00186H |
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Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
calindol | 784 | None | 4 | Mouse | Functional | pIC50 | ~ | - | 5.00 | -27 | 3 | 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 | 300.2 | 4 | 2 | 1 | 5.17 | C[C@@H](NCc1cc2ccccc2[nH]1)c1cccc2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/19836834 | |
CHEMBL3347673 | 115317 | None | 0 | Mouse | Functional | EC50 | = | 77400.00 | 4.11 | - | 1 | Agonist activity at mouse GPRC6A expressed in human tsA201 cells coexpressing GalphaqG66D after 30 mins by inositol phosphate turnover assay | ChEMBL | 186.1 | 4 | 5 | 3 | -1.34 | N=C(N)NCC[C@H]1C[C@@]1(N)C(=O)O | https://dx.doi.org/10.1039/C1MD00186H | |
CHEMBL3633650 | 124172 | None | 12 | Mouse | Functional | IC50 | = | 21877.62 | 4.66 | 1 | 2 | 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 assay | ChEMBL | 391.2 | 6 | 1 | 4 | 2.81 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633650 | 124172 | None | 12 | Mouse | Functional | IC50 | = | 21900.00 | 4.66 | 1 | 2 | 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 assay | ChEMBL | 391.2 | 6 | 1 | 4 | 2.81 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633651 | 124173 | None | 0 | Mouse | Functional | IC50 | = | 39810.72 | 4.40 | - | 1 | 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 assay | ChEMBL | 409.2 | 6 | 1 | 4 | 2.95 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633651 | 124173 | None | 0 | Mouse | Functional | IC50 | = | 39800.00 | 4.40 | - | 1 | 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 assay | ChEMBL | 409.2 | 6 | 1 | 4 | 2.95 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccc(F)cc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633654 | 124174 | None | 0 | Mouse | Functional | IC50 | = | 66069.34 | 4.18 | - | 1 | 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 assay | ChEMBL | 421.2 | 7 | 1 | 5 | 2.82 | COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633654 | 124174 | None | 0 | Mouse | Functional | IC50 | = | 66100.00 | 4.18 | - | 1 | 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 assay | ChEMBL | 421.2 | 7 | 1 | 5 | 2.82 | COc1ccc2[nH]c(-c3ccccc3)c(C(=O)CN(C)CC(=O)N3CCOCC3)c2c1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633655 | 124175 | None | 0 | Mouse | Functional | IC50 | = | 21379.62 | 4.67 | - | 1 | 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 assay | ChEMBL | 409.2 | 6 | 1 | 4 | 2.95 | CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633655 | 124175 | None | 0 | Mouse | Functional | IC50 | = | 21300.00 | 4.67 | - | 1 | 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 assay | ChEMBL | 409.2 | 6 | 1 | 4 | 2.95 | CN(CC(=O)c1c(-c2ccc(F)cc2)[nH]c2ccccc12)CC(=O)N1CCOCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633656 | 124176 | None | 0 | Mouse | Functional | IC50 | = | 9332.54 | 5.03 | 1 | 5 | 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 assay | ChEMBL | 421.2 | 7 | 1 | 5 | 2.82 | COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633656 | 124176 | None | 0 | Mouse | Functional | IC50 | = | 9330.00 | 5.03 | 1 | 5 | 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 assay | ChEMBL | 421.2 | 7 | 1 | 5 | 2.82 | COc1ccc(-c2[nH]c3ccccc3c2C(=O)CN(C)CC(=O)N2CCOCC2)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633663 | 124177 | None | 0 | Mouse | Functional | IC50 | = | 5495.41 | 5.26 | 2 | 2 | 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 assay | ChEMBL | 431.2 | 5 | 1 | 4 | 3.59 | O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633663 | 124177 | None | 0 | Mouse | Functional | IC50 | = | 5500.00 | 5.26 | 2 | 2 | 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 assay | ChEMBL | 431.2 | 5 | 1 | 4 | 3.59 | O=C(CN1CCCC(C(=O)N2CCOCC2)C1)c1c(-c2ccccc2)[nH]c2ccccc12 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633664 | 124178 | None | 4 | Mouse | Functional | IC50 | = | 57543.99 | 4.24 | - | 1 | 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 assay | ChEMBL | 375.2 | 6 | 1 | 3 | 3.57 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633664 | 124178 | None | 4 | Mouse | Functional | IC50 | = | 57300.00 | 4.24 | - | 1 | 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 assay | ChEMBL | 375.2 | 6 | 1 | 3 | 3.57 | CN(CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12)CC(=O)N1CCCC1 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633665 | 124179 | None | 0 | Mouse | Functional | IC50 | = | 6165.95 | 5.21 | 8 | 2 | 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 assay | ChEMBL | 377.2 | 7 | 1 | 4 | 3.28 | CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
CHEMBL3633665 | 124179 | None | 0 | Mouse | Functional | IC50 | = | 6170.00 | 5.21 | 8 | 2 | 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 assay | ChEMBL | 377.2 | 7 | 1 | 4 | 3.28 | CN(CCN1CCOCC1)CC(=O)c1c(-c2ccccc2)[nH]c2ccccc12 | https://dx.doi.org/10.1021/acs.jmedchem.5b01254 | |
glycine | 1826 | None | 72 | Human | Functional | pEC50 | None | - | 3.60 | -12302 | 2 | Unclassified | Guide to Pharmacology | 75.0 | 1 | 2 | 2 | -0.97 | NCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/15576628 | |
L-alanine | 2270 | None | 0 | Human | Functional | pEC50 | None | - | 3.80 | - | 1 | Unclassified | Guide to Pharmacology | 89.0 | 1 | 2 | 2 | -0.58 | C[C@H](N)C(=O)O | https://pubmed.ncbi.nlm.nih.gov/15576628 |
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