AZ2158 [Ligand Id: 14148] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1934424
  • FPR1/Formyl peptide receptor 1 in Human [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
GtoPdb - - 7.7 pKd 19.95 nM Kd Bioorg Med Chem Lett (2012) 22: 532-6 [PMID:22094028]
ChEMBL Antagonist activity at FPR1 in human neutrophils assessed as AB/fMLF-stimulated upregulation of CD11b expression preincubated for 30 mins before AB/FMLF challenge measured after 50 mins using FITC staining by flow cytometry F 7.7 pKd 19.95 nM Kd Bioorg Med Chem Lett (2012) 22: 532-536 [PMID:22094028]
ChEMBL Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay F 8.4 pIC50 3.98 nM IC50 Bioorg Med Chem Lett (2012) 22: 532-536 [PMID:22094028]

ChEMBL data shown on this page come from version 35:

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]