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/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 kappa B subunit 1/nuclear factor kappa B subunit 2/RELA proto-oncogene, NF-kB subunit/Nuclear factor NF-kappa-B complex in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094258] [GtoPdb: 3281, 3282, 3280] [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 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]
