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Assay Detail

CHEMBL2049907

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Functional
Agonist activity against mouse S1P1 assessed as accumulation of cAMP by HTRF assay
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL1914262)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Fused tricyclic indoles as S1P₁ agonists with robust efficacy in animal models of autoimmune disease.
Buzard DJ, Han S, Lopez L, Kawasaki A, Moody J, Thoresen L, Ullman B, Lehmann J, Calderon I, Zhu X, Gharbaoui T, Sengupta D, Krishnan A, Gao Y, Edwards J, Barden J, Morgan M, Usmani K, Chen C, Sadeque A, Thatte J, Solomon M, Fu L, Whelan K, Liu L, Al-Shamma H, Gatlin J, Le M, Xing C, Espinola S, Jones RM.
Bioorg Med Chem Lett (2012) 22 : 4404 -4409
PubMed 22633692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.55 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2048293 2 9.28
CHEMBL2048287 2 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2048293 EC50 = 0.52 nM 9.28
CHEMBL2048287 EC50 = 2.6 nM 8.59
CHEMBL2048293 EC50 = 5.5 nM 8.26
CHEMBL2048287 EC50 = 8.3 nM 8.08