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Assay Detail

CHEMBL1920390

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Functional
Agonist activity at human S1P1 receptor
3
Total Activities
3
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

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 3 7.54 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916400 1 8.17
CHEMBL1916402 1 8.03
CHEMBL1916401 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916400 EC50 = 6.7 nM 8.17
CHEMBL1916402 EC50 = 9.4 nM 8.03
CHEMBL1916401 EC50 = 372.0 nM 6.43