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Assay Detail

CHEMBL864690

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

Binding
Displacement of [33P]S1P from human S1P3 receptor expressed in CHO cells
12
Total Activities
11
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

2-Aryl(pyrrolidin-4-yl)acetic acids are potent agonists of sphingosine-1-phosphate (S1P) receptors.
Yan L, Budhu R, Huo P, Lynch CL, Hale JJ, Mills SG, Hajdu R, Keohane CA, Rosenbach MJ, Milligan JA, Shei GJ, Chrebet G, Bergstrom J, Card D, Mandala SM.
Bioorg Med Chem Lett (2006) 16 : 3564 -3568
PubMed 16621543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.78 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208648 1 6.34
CHEMBL425563 1 6.28
CHEMBL208838 2 6.16
CHEMBL378061 1 5.82
CHEMBL377855 1 5.68
CHEMBL377828 1 5.51
CHEMBL377968 1 5.32
CHEMBL194419 1 4.92
CHEMBL425602 1 -
CHEMBL211006 1 -
CHEMBL378300 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208648 IC50 = 460.0 nM 6.34
CHEMBL425563 IC50 = 530.0 nM 6.28
CHEMBL208838 IC50 = 690.0 nM 6.16
CHEMBL208838 IC50 = 1100.0 nM 5.96
CHEMBL378061 IC50 = 1500.0 nM 5.82
CHEMBL377855 IC50 = 2100.0 nM 5.68
CHEMBL377828 IC50 = 3100.0 nM 5.51
CHEMBL377968 IC50 = 4800.0 nM 5.32
CHEMBL194419 IC50 = 12000.0 nM 4.92
CHEMBL425602 IC50 > 1000.0 nM -
CHEMBL211006 IC50 > 1000.0 nM -
CHEMBL378300 IC50 > 1000.0 nM -