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Assay Detail

CHEMBL4836068

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

Binding
Displacement of radio labeled-SIP from human recombinant S1P2 receptor expressed in CHO cell membranes measured after 15 mins by radioligand based competition binding assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 2 (CHEMBL2955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.
Mammoliti O, Palisse A, Joannesse C, El Bkassiny S, Allart B, Jaunet A, Menet C, Coornaert B, Sonck K, Duys I, Clément-Lacroix P, Oste L, Borgonovi M, Wakselman E, Christophe T, Houvenaghel N, Jans M, Heckmann B, Sanière L, Brys R.
J Med Chem (2021) 64 : 6037 -6058
PubMed 33939425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.39 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852127 1 6.72
CHEMBL4860509 1 6.52
CHEMBL4867313 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852127 IC50 = 190.0 nM 6.72
CHEMBL4860509 IC50 = 300.0 nM 6.52
CHEMBL4867313 IC50 = 1200.0 nM 5.92