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

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ChEMBL ligand: CHEMBL267179
  • 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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  • FPR3/N-formyl peptide receptor 3 in Human [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089]
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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]
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]
ChEMBL GPCR PRESTO-Tango dose-response in agonist mode with target: FPR1 F 8.43 pEC50 3.69 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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/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]
FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089]
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]

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]