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 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]