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Assay Detail

CHEMBL1108114

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

Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor expressed in HEK293T cells after 60 mins by scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 4 (CHEMBL3230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Bernier SG, Doyle E, Kavarana MJ, Satz AL, Lorusso J, Blanchette HS, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett (2010) 20 : 2520 -2524
PubMed 20304639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.31 8.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225155 1 8.98
CHEMBL1093429 1 8.47
CHEMBL1093823 1 8.36
CHEMBL514170 1 8.31
CHEMBL1090829 1 8.19
CHEMBL475405 1 7.99
CHEMBL1090796 1 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225155 IC50 = 1.04 nM 8.98
CHEMBL1093429 IC50 = 3.4 nM 8.47
CHEMBL1093823 IC50 = 4.4 nM 8.36
CHEMBL514170 IC50 = 4.87 nM 8.31
CHEMBL1090829 IC50 = 6.5 nM 8.19
CHEMBL475405 IC50 = 10.3 nM 7.99
CHEMBL1090796 IC50 = 13.1 nM 7.88