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ChEMBL ligand: CHEMBL20943 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7] | ||||||||
ChEMBL | Displacement of [3H]DTG from sigma2 receptor in rat liver membranes after 60 mins by liquid scintillation counting method | B | 7.2 | pKi | 63.4 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
ChEMBL | Displacement of (+)-[3H]pentazocine from sigma1 receptor in rat brain membranes after 60 mins by liquid scintillation counting method | B | 7.56 | pKi | 27.4 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
ChEMBL | Displacement of (+)-[3H]pentazocine from sigma1 receptor in Sprague-Dawley rat cerebral membrane after 90 mins by liquid scintillation counting | B | 7.66 | pKi | 22.1 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
Vesicular acetylcholine transporter in Torpedo californica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3313] [UniProtKB: P81721] | ||||||||
ChEMBL | Displacement of [3H]vesamicol from Vesamicol receptor of Torpedo californica | B | 7.47 | pIC50 | 34 | nM | IC50 | J Med Chem (1991) 34: 2638-2643 [PMID:1875353] |
Vesicular acetylcholine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4767] [GtoPdb: 1013] [UniProtKB: Q16572] | ||||||||
GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | Biochem Pharmacol (1995) 49: 791-7 [PMID:7702637] |
ChEMBL | Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (1989) 32: 1217-1230 [PMID:2724295] |
ChEMBL | Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1989) 32: 1217-1230 [PMID:2724295] |
Vesicular acetylcholine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2125] [GtoPdb: 1013] [UniProtKB: Q62666] | ||||||||
ChEMBL | Displacement of (-)-[3H]vesamicol from rat VAChT expressed in rat PC12 cell membranes after 60 mins by liquid scintillation counting method | B | 7.31 | pKi | 48.6 | nM | Ki | J Med Chem (2018) 61: 6937-6943 [PMID:29969030] |
ChEMBL | Displacement of (-)-[3H]vesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 60 mins by liquid scintillation counting in presence of DTG | B | 7.47 | pKi | 33.9 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
ChEMBL | Displacement of [125I]O-iodo-trans-decalinvesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 1 hr by gamma counting | B | 7.48 | pKi | 32.9 | nM | Ki | Bioorg Med Chem (2012) 20: 4936-4941 [PMID:22831799] |
ChEMBL data shown on this page come from version 32:
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]