PF-06282999 [Ligand Id: 10053] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3633460 (Pf-06282999)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164]
ChEMBL Inhibition of peroxidase activity of MPO isolated from human polynuclear leukocytes using Amplex Red as substrate assessed as formation of resorufin measured every 20 secs by spectrophotometric analysis B 6.5 pKi 316.23 nM Ki J Med Chem (2015) 58: 8513-8528 [PMID:26509551]
GtoPdb Inhibition of the peroxidase activity of MPO isolated from human polynuclear leukocytes. - 6.5 pKi 316 nM Ki J Med Chem (2015) 58: 8513-28 [PMID:26509551]
ChEMBL Irreversible inhibition of MPO in LPS-stimulated human whole blood after 4 hrs by Amplex Red/H2O2-based fluorescence plate reader analysis B 5.72 pIC50 1900 nM IC50 J Med Chem (2015) 58: 8513-8528 [PMID:26509551]

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]