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Assay Detail

CHEMBL1920395

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Functional
Agonist activity at rat S1P1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL1914263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists.
Buzard D, Han S, Thoresen L, Moody J, Lopez L, Kawasaki A, Schrader T, Sage C, Gao Y, Edwards J, Barden J, Thatte J, Fu L, Solomon M, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM.
Bioorg Med Chem Lett (2011) 21 : 6013 -6018
PubMed 21852130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.95 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916399 1 9.00
CHEMBL1916559 1 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916399 EC50 = 1.0 nM 9.00
CHEMBL1916559 EC50 = 1.3 nM 8.89