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Assay Detail

CHEMBL806183

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

Binding
Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sphingosine 1-phosphate receptor 3 (CHEMBL3892)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent S1P receptor agonists replicate the pharmacologic actions of the novel immune modulator FTY720.
Hale JJ, Neway W, Mills SG, Hajdu R, Ann Keohane C, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Koo GC, Koprak SL, Jackson JJ, Rosen H, Mandala S.
Bioorg Med Chem Lett (2004) 14 : 3351 -3355
PubMed 15149705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.09 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225155 1 10.40
CHEMBL432067 1 9.15
CHEMBL114606 1 8.20
CHEMBL115554 1 7.75
CHEMBL113344 1 7.21
CHEMBL112655 1 7.17
CHEMBL115713 1 7.07
CHEMBL325198 1 6.55
CHEMBL114976 1 6.50
CHEMBL115714 1 6.50
CHEMBL114584 1 6.29
CHEMBL91283 1 6.14
CHEMBL325050 1 5.18
CHEMBL115131 1 5.12
CHEMBL326346 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225155 IC50 = 0.04 nM 10.40
CHEMBL432067 IC50 = 0.71 nM 9.15
CHEMBL114606 IC50 = 6.3 nM 8.20
CHEMBL115554 IC50 = 18.0 nM 7.75
CHEMBL113344 IC50 = 62.0 nM 7.21
CHEMBL112655 IC50 = 68.0 nM 7.17
CHEMBL115713 IC50 = 85.0 nM 7.07
CHEMBL325198 IC50 = 280.0 nM 6.55
CHEMBL114976 IC50 = 320.0 nM 6.50
CHEMBL115714 IC50 = 320.0 nM 6.50
CHEMBL114584 IC50 = 510.0 nM 6.29
CHEMBL91283 IC50 = 720.0 nM 6.14
CHEMBL325050 IC50 = 6600.0 nM 5.18
CHEMBL115131 IC50 = 7600.0 nM 5.12
CHEMBL326346 IC50 > 10000.0 nM -