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Assay Detail

CHEMBL1029040

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Functional
Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgammaS binding
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Bernier SG, Kavarana MJ, Doyle E, Lorusso J, Kelley MS, Halley K, Hutchings A, Wright AD, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett (2009) 19 : 369 -372
PubMed 19081720 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.83 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473269 1 9.35
CHEMBL474689 1 9.26
CHEMBL515921 1 8.96
CHEMBL474688 1 8.68
CHEMBL475495 1 8.62
CHEMBL225155 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473269 EC50 = 0.45 nM 9.35
CHEMBL474689 EC50 = 0.55 nM 9.26
CHEMBL515921 EC50 = 1.1 nM 8.96
CHEMBL474688 EC50 = 2.1 nM 8.68
CHEMBL475495 EC50 = 2.4 nM 8.62
CHEMBL225155 EC50 = 7.9 nM 8.10