pyrazolone, 1 [Ligand Id: 5831] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL379761
  • FPR1/Formyl peptide receptor 1 in Human [ChEMBL: CHEMBL3359] [GtoPdb: 222] [UniProtKB: P21462]
  • FPR1 in Mouse [GtoPdb: 222] [UniProtKB: P33766]
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  • FPR2/ALX/Lipoxin A4 receptor in Human [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
  • FPR2/ALX in Mouse [GtoPdb: 223] [UniProtKB: O88536]
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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 Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay B 7.29 pEC50 51.29 nM EC50 J Med Chem (2019) 62: 5242-5248 [PMID:31038950]
ChEMBL Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay F 7.49 pEC50 32.36 nM EC50 J Med Chem (2019) 62: 5242-5248 [PMID:31038950]
FPR1 in Mouse [GtoPdb: 222] [UniProtKB: P33766]
GtoPdb - - 8.7 pEC50 - - - Mol Pharmacol (2013) 83: 389-98 [PMID:23160941]
FPR2/ALX/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
ChEMBL Biased agonist activity at human FPR2 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay F 7.02 pEC50 95.5 nM EC50 J Med Chem (2019) 62: 5242-5248 [PMID:31038950]
ChEMBL Activity at human FPRL1-mediated calcium mobilization in CHO cells F 7.36 pEC50 44 nM EC50 Bioorg Med Chem Lett (2006) 16: 3713-3718 [PMID:16697190]
ChEMBL Agonist activity at human recombinant FPRL1 expressed in CHO cells assessed as calcium flux by aequorin based bioluminescence assay F 7.36 pEC50 44 nM EC50 Bioorg Med Chem Lett (2007) 17: 6633-6637 [PMID:17920884]
ChEMBL Biased agonist activity at human FPR2 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay B 7.39 pEC50 40.74 nM EC50 J Med Chem (2019) 62: 5242-5248 [PMID:31038950]
GtoPdb - - 7.4 pEC50 - - - Bioorg Med Chem Lett (2006) 16: 3713-8 [PMID:16697190]
FPR2/ALX in Mouse [GtoPdb: 223] [UniProtKB: O88536]
GtoPdb - - 6.92 pEC50 - - - Mol Pharmacol (2013) 83: 389-98 [PMID:23160941]

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]