LXA4 [Ligand Id: 1034] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL392438 |
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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: P19838, Q00653, Q04206] | ||||||||
| 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 33:
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]
