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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 |
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]