W54011 [Ligand Id: 581] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628668
  • C5a1 receptor/C5a anaphylatoxin chemotactic receptor in Human [ChEMBL: CHEMBL2373] [GtoPdb: 32] [UniProtKB: P21730]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
C5a1 receptor/C5a anaphylatoxin chemotactic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2373] [GtoPdb: 32] [UniProtKB: P21730]
GtoPdb - - 8.7 pKi - - - J Biol Chem (2002) 277: 49403-7 [PMID:12384495]
ChEMBL Antagonist activity at C5aR1 in HMDM assessed as inhibition of 1 nM recombinant human C5a-induced intracellular calcium release preincubated for 1 hr followed by human C5a-induction and measured after 60 hrs by FLIPR assay F 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL Antagonist activity at C5aR1 in human neutrophils assessed as inhibition of 0.1 nM recombinant human C5a-induced intracellular calcium release F 8.7 pIC50 2 nM IC50 J Med Chem (2018) 61: 3253-3276 [PMID:28977749]

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]