Initializing potency table...
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 | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
CANNABIDIVARIN | 90652 | None | 24 | Human | Binding | EC50 | = | 2400.00 | 5.62 | - | 5 | Binding affinity to human GPR6 expressed in HEK293 cells assessed as reduction in cAMP level incubated for 1 hr by HTRF assay | ChEMBL | 286.2 | 4 | 2 | 2 | 5.07 | C=C(C)[C@@H]1CCC(C)=C[C@H]1c1c(O)cc(CCC)cc1O | https://dx.doi.org/10.1021/acs.jnatprod.0c00965 | |
CHEMBL3962956 | 151623 | None | 8 | Human | Binding | Ki | = | 6.00 | 8.22 | - | 1 | Binding affinity to GPR6 (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting based competition binding assay | ChEMBL | 473.2 | 5 | 1 | 7 | 2.91 | CC(=O)N1CCc2nc(N3CCC(Oc4ccc(F)cc4F)CC3)c(N[C@H]3CCOC3)nc2C1 | - | |
CHEMBL4598390 | 176795 | None | 0 | Human | Binding | Ki | = | 7.00 | 8.15 | - | 1 | Displacement of 3H-RL338 from human GPR6 expressed in T-REx-CHO-GPR6 cells assessed as inhibition constant by competition binding assay | ChEMBL | 396.2 | 5 | 1 | 6 | 3.20 | Fc1ccc(CN2CCN(c3nc4cnccc4nc3NC3CC3)CC2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.0c02081 | |
CHEMBL5093828 | 217936 | None | 0 | Human | Binding | Ki | = | 16.00 | 7.80 | - | 1 | Displacement of 3H-RL338 from human GPR6 expressed in T-REx-CHO-GPR6 cells assessed as inhibition constant by competition binding assay | ChEMBL | - | - | - | - | - | CC(=O)N1C=Cc2nc(N3CCC(Oc4ccc(F)cc4F)CC3)c(NC(C)C)nc2C1 | https://dx.doi.org/10.1021/acs.jmedchem.0c02081 | |
CHEMBL5410506 | 195773 | None | 0 | Human | Binding | Kd | = | 66.07 | 7.18 | 7 | 2 | Specific binding affinity to full-length wild-type human brain GPR6 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay | ChEMBL | 920.4 | 19 | 2 | 12 | 9.56 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | https://dx.doi.org/10.1021/acs.jmedchem.3c01707 | |
CHEMBL5410506 | 195773 | None | 0 | Human | Binding | IC50 | = | 213.80 | 6.67 | 7 | 2 | Competitive total binding affinity to full-length wild-type human brain GPR6 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of CVN424 by NanoBRET assay | ChEMBL | 920.4 | 19 | 2 | 12 | 9.56 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | https://dx.doi.org/10.1021/acs.jmedchem.3c01707 | |
CHEMBL5410506 | 195773 | None | 0 | Human | Binding | Ki | = | 13.18 | 7.88 | 7 | 2 | Competitive total binding affinity to full-length wild-type human brain GPR6 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of CVN424 by NanoBRET assay | ChEMBL | 920.4 | 19 | 2 | 12 | 9.56 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | https://dx.doi.org/10.1021/acs.jmedchem.3c01707 | |
CVN424 | 1223 | None | 16 | Human | Binding | pKi | = | - | 8.03 | - | 1 | Unclassified | Guide to Pharmacology | 473.2 | 5 | 1 | 7 | 2.91 | CC(=O)N1CCc2nc(N3CCC(Oc4ccc(F)cc4F)CC3)c(N[C@@H]3CCOC3)nc2C1 | https://pubmed.ncbi.nlm.nih.gov/33861086 | |
CVN424 | 1223 | None | 16 | Human | Binding | Ki | = | 9.40 | 8.03 | - | 1 | Displacement of 3H-RL338 from human GPR6 expressed in T-REx-CHO-GPR6 cells assessed as inhibition constant by competition binding assay | ChEMBL | 473.2 | 5 | 1 | 7 | 2.91 | CC(=O)N1CCc2nc(N3CCC(Oc4ccc(F)cc4F)CC3)c(N[C@@H]3CCOC3)nc2C1 | https://dx.doi.org/10.1021/acs.jmedchem.0c02081 | |
CVN424 | 1223 | None | 16 | Human | Binding | Ki | = | 5.50 | 8.26 | - | 1 | Binding affinity to GPR6 (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting based competition binding assay | ChEMBL | 473.2 | 5 | 1 | 7 | 2.91 | CC(=O)N1CCc2nc(N3CCC(Oc4ccc(F)cc4F)CC3)c(N[C@@H]3CCOC3)nc2C1 | - |
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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 | |