(-)-pentazocine [Ligand Id: 1606] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL560 (Pentazocine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]; J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330] |
| ChEMBL | Binding affinity to kappa opioid receptor (unknown origin) | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity to mu opioid receptor (unknown origin) | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
| ChEMBL | Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membrane incubated for 120 mins by liquid scintillation counting method | B | 8.24 | pKi | 5.7 | nM | Ki | Eur J Med Chem (2021) 210: 112950-112950 [PMID:33148494] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane measured after 120 mins by solid scintillation counting method | B | 8.24 | pKi | 5.7 | nM | Ki | Eur J Med Chem (2021) 219: 113443-113443 [PMID:33901806] |
| ChEMBL | Displacement of [3H]-pentazocine from guinea pig brain sigma 1 receptor incubated for 120 mins by liquid scintillation counting method | B | 8.27 | pKi | 5.4 | nM | Ki | RSC Med Chem (2021) 12: 237-244 [PMID:34046612] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | B | 8.33 | pKi | 4.7 | nM | Ki | ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
| ChEMBL | Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes measured after 120 mins by scintillation counting method | B | 8.41 | pKi | 3.93 | nM | Ki | Eur J Med Chem (2022) 228: 114038-114038 [PMID:34902734] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | Binding affinity to sigma-2 receptor (unknown origin) | B | 5.73 | pKi | 1880 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| ChEMBL | Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor (unknown origin) incubated for 1 hr in presence of (+)SKF10047 by liquid scintillation counting method | B | 5.83 | pKi | 1465 | nM | Ki | ACS Med Chem Lett (2020) 11: 889-894 [PMID:32435401] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity to sigma-1 receptor (unknown origin) | B | 7.92 | pKi | 12.1 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| δ receptor in Human [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| GtoPdb | - | - | 7.3 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
