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ChEMBL ligand: CHEMBL513922 (AC-5216, Emapunil, Emapunilo, 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 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]