GR 89696 [Ligand Id: 1649] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL603370 (GR-89696) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | In vitro inhibitory activity against delta specific tissue of hamster vas deferens | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) | B | 6.44 | pKi | 360 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor | B | 9.35 | pKi | 0.45 | nM | Ki | Eur J Med Chem (2011) 46: 1972-1982 [PMID:21481987] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - | Nucl Med Biol (2002) 29: 47-53 [PMID:11786275] |
| ChEMBL | In vitro agonist activity at kappa opioid receptor in rabbit vas deferens. | F | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
| ChEMBL | In vitro agonist activity at kappa opioid receptor in rabbit vas deferens. | F | 10.39 | pIC50 | 0.04 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
| ChEMBL | In vitro agonist activity at kappa opioid receptor in rabbit vas deferens. | F | 10.74 | pIC50 | 0.02 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Agonist activity at KOR in mouse vas deferens assessed as inhibition of electrically evoked vas deferens contraction | F | 10.39 | pIC50 | 0.04 | nM | IC50 | Eur J Med Chem (2022) 243: 114785-114785 [PMID:36179400] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay | B | 9.34 | pKi | 0.46 | nM | Ki | Eur J Med Chem (2022) 230: 114079-114079 [PMID:35033825] |
| ChEMBL | Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting | B | 9.44 | pKi | 0.36 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5326-5330 [PMID:26411794] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [(3)H]U69593 from mu opioid receptor | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (2010) 53: 4212-4222 [PMID:20441176] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | In vitro inhibitory activity against mu specific tissue of rat vas deferens | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1993) 36: 2075-2083 [PMID:8393489] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
