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Assay Detail

CHEMBL1108118

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

Functional
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
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
EC50 7 8.46 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475405 1 9.28
CHEMBL1093429 1 8.84
CHEMBL1093823 1 8.79
CHEMBL514170 1 8.66
CHEMBL225155 1 8.25
CHEMBL1090796 1 7.74
CHEMBL1090829 1 7.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475405 EC50 = 0.52 nM 9.28
CHEMBL1093429 EC50 = 1.44 nM 8.84
CHEMBL1093823 EC50 = 1.62 nM 8.79
CHEMBL514170 EC50 = 2.2 nM 8.66
CHEMBL225155 EC50 = 5.6 nM 8.25
CHEMBL1090796 EC50 = 18.3 nM 7.74
CHEMBL1090829 EC50 = 22.4 nM 7.65