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ChEMBL ligand: CHEMBL513922 (AC-5216, Emapunil, XBD-173, XBD173) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Translocator protein in Human [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
GtoPdb | Affinity for the low affinity TSPO binding site in human brain tissue | - | 7.52 | pKi | 30.3 | nM | Ki | Synapse (2011) 65: 257-9 [PMID:21132812] |
GtoPdb | Affinity for the high affinity TSPO binding site in human brain tissue | - | 8.62 | pKi | 2.4 | nM | Ki | Synapse (2011) 65: 257-9 [PMID:21132812] |
Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
ChEMBL | Displacement of [11C]-PK-11195 from TPSO in Sprague-Dawley rat brain homogenate after 30 mins by gamma counting | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2011) 54: 6040-6049 [PMID:21790126] |
ChEMBL | Displacement of [11C]PK11195 from PBR receptor in rat brain membrane | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1707-1710 [PMID:19217778] |
GtoPdb | - | - | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1707-10 [PMID:19217778] |
Translocator protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5742] [GtoPdb: 2879] [UniProtKB: P30536] | ||||||||
ChEMBL | Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293T cell membranes after 90 mins by scintillation counting method | B | 7.5 | pKi | 31.3 | nM | Ki | Medchemcomm (2017) 8: 202-210 [PMID:30108706] |
GtoPdb | Affinity for the low affinity TSPO binding site in human brain tissue | - | 7.52 | pKi | 30.3 | nM | Ki | Synapse (2011) 65: 257-9 [PMID:21132812] |
ChEMBL | Displacement of [3H]PK11195 from human wild type TSPO expressed in HEK293T cell membranes after 90 mins by scintillation counting method | B | 8.19 | pKi | 6.4 | nM | Ki | Medchemcomm (2017) 8: 202-210 [PMID:30108706] |
GtoPdb | Affinity for the high affinity TSPO binding site in human brain tissue | - | 8.62 | pKi | 2.4 | nM | Ki | Synapse (2011) 65: 257-9 [PMID:21132812] |
Translocator protein in Rat [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
GtoPdb | - | - | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 1707-10 [PMID:19217778] |
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]