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Assay Detail

CHEMBL913926

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

Functional
Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists.
Hale JJ, Lynch CL, Neway W, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Parent SA, Chrebet G, Bergstrom J, Card D, Ferrer M, Hodder P, Strulovici B, Rosen H, Mandala S.
J Med Chem (2004) 47 : 6662 -6665
PubMed 15615513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.79 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225575 1 9.70
CHEMBL114606 1 9.52
CHEMBL425563 1 9.30
CHEMBL224005 1 9.10
CHEMBL224853 1 8.89
CHEMBL389880 1 8.89
CHEMBL375488 1 8.85
CHEMBL224571 1 8.85
CHEMBL224799 1 8.62
CHEMBL426191 1 8.57
CHEMBL224599 1 8.48
CHEMBL224549 1 8.23
CHEMBL224800 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225575 EC50 = 0.2 nM 9.70
CHEMBL114606 EC50 = 0.3 nM 9.52
CHEMBL425563 EC50 = 0.5 nM 9.30
CHEMBL224005 EC50 = 0.8 nM 9.10
CHEMBL224853 EC50 = 1.3 nM 8.89
CHEMBL389880 EC50 = 1.3 nM 8.89
CHEMBL375488 EC50 = 1.4 nM 8.85
CHEMBL224571 EC50 = 1.4 nM 8.85
CHEMBL224799 EC50 = 2.4 nM 8.62
CHEMBL426191 EC50 = 2.7 nM 8.57
CHEMBL224599 EC50 = 3.3 nM 8.48
CHEMBL224549 EC50 = 5.9 nM 8.23
CHEMBL224800 EC50 = 47.0 nM 7.33