LXA4 [Ligand Id: 1034] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL392438
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  • GPR32 in Human [GtoPdb: 99] [UniProtKB: O75388]
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  • FPR3 in Mouse [GtoPdb: 224] [UniProtKB: O08790]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
FPR2/ALX/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090]
GtoPdb - - 9.3 pKd - - - J Exp Med (1994) 180: 253-60 [PMID:8006586];
J Biol Chem (1992) 267: 16168-76 [PMID:1322894]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation pretreated for 30 mins followed by LPS stimulation for 24 hrs by luciferase reporter gene assay B 7.58 pIC50 26.3 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IFNgamma secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay B 7.65 pIC50 22.2 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-12p70 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay B 7.93 pIC50 11.8 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in TNFalpha secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay B 8.11 pIC50 7.7 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-1beta secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay B 8.74 pIC50 1.8 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
ChEMBL Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-6 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay B 8.77 pIC50 1.7 nM IC50 Eur J Med Chem (2019) 162: 80-108 [PMID:30419493]
GtoPdb - - 12 pEC50 ~0 nM EC50 Proc Natl Acad Sci USA (2010) 107: 1660-5 [PMID:20080636]
Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [UniProtKB: P19838Q00653Q04206]
ChEMBL Inhibition of LPS-induced NF-kappaB activation in human THP-1 monocytes expressing luciferase gene pretreated for 30 mins followed by LPS stimulation and measured after 24 hrs by bioluminescence analysis B 10.22 pIC50 0.06 nM IC50 J Med Chem (2021) 64: 9193-9216 [PMID:34138563]
GPR32 in Human [GtoPdb: 99] [UniProtKB: O75388]
GtoPdb - - 9.7 pEC50 0.2 nM EC50 Proc Natl Acad Sci USA (2010) 107: 1660-5 [PMID:20080636]
FPR3 in Mouse [GtoPdb: 224] [UniProtKB: O08790]
GtoPdb - - 8.82 pKd - - - J Exp Med (1997) 185: 1693-704 [PMID:9151906]

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]