PF-04859989 [Ligand Id: 9038] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2047851 (PF-04859989)
  • Kynurenine/alpha-aminoadipate aminotransferase in Rat [ChEMBL: CHEMBL2662] [UniProtKB: Q64602]
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  • Kynurenine/alpha-aminoadipate aminotransferase, mitochondrial in Human [ChEMBL: CHEMBL2046259] [UniProtKB: Q8N5Z0]
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  • L-Cysteine:2-oxoglutarate aminotransferase/Kynurenine--oxoglutarate transaminase I in Human [ChEMBL: CHEMBL3962] [GtoPdb: 1445] [UniProtKB: Q16773]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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
ChEMBL Inhibition of Kynurenine aminotransferase II (unknown origin) B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2023) 251: 115258-115258 [PMID:36917881]
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 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]