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ChEMBL ligand: CHEMBL2047851 (PF-04859989) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Kynurenine/alpha-aminoadipate aminotransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2662] [UniProtKB: Q64602] | ||||||||
ChEMBL | Inhibition of rat recombinant KAT2 assessed as conversion of L-kynurenine into kynurenic acid after 15 to 20 hrs | B | 6.58 | pIC50 | 263 | nM | IC50 | ACS Med Chem Lett (2012) 3: 187-192 [PMID:24900455] |
Kynurenine/alpha-aminoadipate aminotransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046259] [UniProtKB: Q8N5Z0] | ||||||||
ChEMBL | Irreversible inhibition of human KAT2 using L-kynurenine as substrate measured every 5 mins over 16 hrs by SpectraMax plate reader analysis | B | 7.85 | pKi | 14.2 | nM | Ki | ACS Med Chem Lett (2013) 4: 37-40 [PMID:24900560] |
ChEMBL | Inhibition of KAT2 (unknown origin) | B | 7.85 | pKi | 14.2 | nM | Ki | Medchemcomm (2013) 4: 125-129 |
ChEMBL | Inhibition of human KAT2 using L-kynurenine as substrate after 15 to 20 hrs by UV-visible spectra analysis | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1961-1966 [PMID:23466229] |
ChEMBL | Inhibition of human recombinant KAT2 assessed as conversion of L-kynurenine into kynurenic acid after 15 to 20 hrs | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2012) 3: 187-192 [PMID:24900455] |
ChEMBL | Inhibition of human KAT2 using L-kynurenine as substrate measured after 15-20 hrs by SpectraMax plate reader analysis | B | 7.64 | pIC50 | 23 | nM | IC50 | ACS Med Chem Lett (2013) 4: 37-40 [PMID:24900560] |
ChEMBL | Inhibition of KAT2 (unknown origin) | B | 7.64 | pIC50 | 23 | nM | IC50 | Medchemcomm (2013) 4: 125-129 |
Kynurenine--oxoglutarate transaminase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046260] [UniProtKB: Q6YP21] | ||||||||
ChEMBL | Inhibition of human KAT3 | B | 4.96 | pIC50 | 11000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 187-192 [PMID:24900455] |
ChEMBL | Inhibition of human KAT3 using L-kynurenine as substrate measured after 24 hrs by SpectraMax plate reader analysis | B | 5.04 | pIC50 | 9040 | nM | IC50 | ACS Med Chem Lett (2013) 4: 37-40 [PMID:24900560] |
L-Cysteine:2-oxoglutarate aminotransferase/Kynurenine--oxoglutarate transaminase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3962] [GtoPdb: 1445] [UniProtKB: Q16773] | ||||||||
ChEMBL | Inhibition of human KAT1 using L-kynurenine as substrate measured after 16 hrs by SpectraMax plate reader analysis | B | 4.52 | pIC50 | 30400 | nM | IC50 | ACS Med Chem Lett (2013) 4: 37-40 [PMID:24900560] |
ChEMBL | Inhibition of human KAT1 | B | 4.66 | pIC50 | 22000 | nM | IC50 | ACS Med Chem Lett (2012) 3: 187-192 [PMID:24900455] |
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]