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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]