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Assay Detail

CHEMBL4383710

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

N-formyl peptide receptor 2 (CHEMBL4227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Asymmetric synthesis and biological evaluation of imidazole- and oxazole-containing synthetic lipoxin A<sub>4</sub> mimetics (sLXms).
de Gaetano M, Butler E, Gahan K, Zanetti A, Marai M, Chen J, Cacace A, Hams E, Maingot C, McLoughlin A, Brennan E, Leroy X, Loscher CE, Fallon P, Perretti M, Godson C, Guiry PJ.
Eur J Med Chem (2019) 162 : 80 -108
PubMed 30419493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.45 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4462922 1 9.15
CHEMBL4436717 1 9.05
CHEMBL4440913 1 8.66
CHEMBL4434857 1 8.60
CHEMBL4551559 1 8.37
CHEMBL4536276 1 8.36
CHEMBL4574711 1 7.73
CHEMBL392438 LIPOXIN A4 1 7.65
CHEMBL4582724 1 -
CHEMBL4534051 1 -
CHEMBL4460558 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4462922 IC50 = 0.7 nM 9.15
CHEMBL4436717 IC50 = 0.9 nM 9.05
CHEMBL4440913 IC50 = 2.2 nM 8.66
CHEMBL4434857 IC50 = 2.5 nM 8.60
CHEMBL4551559 IC50 = 4.3 nM 8.37
CHEMBL4536276 IC50 = 4.4 nM 8.36
CHEMBL4574711 IC50 = 18.5 nM 7.73
CHEMBL392438 LIPOXIN A4 IC50 = 22.2 nM 7.65
CHEMBL4582724 IC50 - -
CHEMBL4534051 IC50 - -
CHEMBL4460558 IC50 - -