fMet-Leu-Phe [Ligand Id: 1022] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267179
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  • FPR1/Formyl peptide receptor 1 in Human [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
  • FPR1 in Mouse [GtoPdb: 222] [UniProtKB: P33766]
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  • FPR3/Formyl peptide receptor-related sequence 1 in Mouse [ChEMBL: CHEMBL3407315] [GtoPdb: 224] [UniProtKB: O08790]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FML2_HUMAN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [UniProtKB: Q6L5J4]
ChEMBL Agonist activity at FPRL2 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay F 5.72 pEC50 1900 nM EC50 J Med Chem (2009) 52: 5044-5057 [PMID:19639995]
FPR1/Formyl peptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
ChEMBL Binding affinity to human FPR1 receptor B 8.52 pKd 3 nM Kd J Med Chem (2015) 58: 1089-1099 [PMID:25587631]
ChEMBL Displacement of [3H]-fMLP from FPR in human neutrophils B 7.38 pKi 42 nM Ki Bioorg Med Chem Lett (2007) 17: 3696-3701 [PMID:17475488]
ChEMBL Binding affinity towards fMLF receptor using human neutrophils B 7.7 pIC50 20 nM IC50 J Med Chem (1996) 39: 1013-1015 [PMID:8676333]
ChEMBL Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils F 7.7 pEC50 20 nM EC50 J Med Chem (1996) 39: 1013-1015 [PMID:8676333]
ChEMBL Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay F 8 pEC50 10 nM EC50 J Med Chem (2009) 52: 5044-5057 [PMID:19639995]
GtoPdb - - 10.2 pEC50 - - - J Exp Med (1976) 143: 1154-69 [PMID:1262785];
Biochemistry (1980) 19: 2404-10 [PMID:7387981]
FPR1 in Mouse [GtoPdb: 222] [UniProtKB: P33766]
GtoPdb - - 4.7 pEC50 - - - J Exp Med (1999) 190: 741-7 [PMID:10477558];
J Immunol (2008) 181: 1429-37 [PMID:18606697]
FPR3/Formyl peptide receptor-related sequence 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3407315] [GtoPdb: 224] [UniProtKB: O08790]
ChEMBL Binding affinity to mouse FPR2 receptor B 6.52 pKd >300 nM Kd J Med Chem (2015) 58: 1089-1099 [PMID:25587631]
FPR2/ALX/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
GtoPdb - - 6.37 pKd - - - J Biol Chem (1993) 268: 18167-75 [PMID:8349692]
ChEMBL Binding affinity to human FPR2 receptor B 6.52 pKd >300 nM Kd J Med Chem (2015) 58: 1089-1099 [PMID:25587631]
ChEMBL Agonist activity at FPRL1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay F 4.69 pEC50 20400 nM EC50 J Med Chem (2009) 52: 5044-5057 [PMID:19639995]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]