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Assay Detail

CHEMBL1108113

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

Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor expressed in HEK293T cells after 60 mins by scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Bernier SG, Doyle E, Kavarana MJ, Satz AL, Lorusso J, Blanchette HS, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett (2010) 20 : 2520 -2524
PubMed 20304639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.35 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225155 1 9.04
CHEMBL514170 1 7.70
CHEMBL475405 1 6.70
CHEMBL1088820 1 6.54
CHEMBL1090828 1 6.16
CHEMBL1089127 1 6.00
CHEMBL1088819 1 5.70
CHEMBL1093823 1 5.70
CHEMBL1093424 1 5.49
CHEMBL1090796 1 5.42
CHEMBL1093429 1 5.35
CHEMBL1092190 1 -
CHEMBL1092191 1 -
CHEMBL1090673 1 -
CHEMBL1090782 1 -
CHEMBL1090829 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225155 IC50 = 0.92 nM 9.04
CHEMBL514170 IC50 = 20.0 nM 7.70
CHEMBL475405 IC50 = 200.0 nM 6.70
CHEMBL1088820 IC50 = 285.0 nM 6.54
CHEMBL1090828 IC50 = 700.0 nM 6.16
CHEMBL1089127 IC50 = 1000.0 nM 6.00
CHEMBL1088819 IC50 = 2000.0 nM 5.70
CHEMBL1093823 IC50 = 2000.0 nM 5.70
CHEMBL1093424 IC50 = 3250.0 nM 5.49
CHEMBL1090796 IC50 = 3800.0 nM 5.42
CHEMBL1093429 IC50 = 4500.0 nM 5.35
CHEMBL1092190 IC50 > 10000.0 nM -
CHEMBL1092191 IC50 > 10000.0 nM -
CHEMBL1090673 IC50 > 1000.0 nM -
CHEMBL1090782 IC50 > 1000.0 nM -
CHEMBL1090829 IC50 > 100000.0 nM -