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

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ChEMBL ligand: CHEMBL3633460 (Pf-06282999)
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  • thyroid peroxidase/Thyroid peroxidase in Human [ChEMBL: CHEMBL1839] [GtoPdb: 2526] [UniProtKB: P07202]
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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 Inhibition of MPO in human HL-60 cells measured after 15 mins in presence of H2O2 by chemiluminescence assay B 4.45 pIC50 35500 nM IC50 J Med Chem (2022) 65: 11485-11496 [PMID:36005476]
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 Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay B 6.73 pIC50 187 nM IC50 J Med Chem (2022) 65: 11485-11496 [PMID:36005476]
thyroid peroxidase/Thyroid peroxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1839] [GtoPdb: 2526] [UniProtKB: P07202]
ChEMBL Inhibition of human recombinant TPO (1 to 839 residues) expressed in baculovirus-infected insect cells measured after 15 mins in presence of H2O2 by chemiluminescence assay B 6 pIC50 990 nM IC50 J Med Chem (2022) 65: 11485-11496 [PMID:36005476]

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]