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Assay Detail

CHEMBL800922

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

Binding
Binding affinity to human sphingosine 1-phosphate receptor 1 expressed in CHO cells was determined by using [33P]-S1P as radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists.
Hale JJ, Doherty G, Toth L, Mills SG, Hajdu R, Keohane CA, Rosenbach M, Milligan J, Shei GJ, Chrebet G, Bergstrom J, Card D, Forrest M, Sun SY, West S, Xie H, Nomura N, Rosen H, Mandala S.
Bioorg Med Chem Lett (2004) 14 : 3501 -3505
PubMed 15177461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 8.89 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118860 1 9.70
CHEMBL119413 1 9.52
CHEMBL333335 1 9.52
CHEMBL441826 1 9.40
CHEMBL119354 1 9.40
CHEMBL119440 1 9.40
CHEMBL119382 1 9.30
CHEMBL331054 1 9.30
CHEMBL323617 1 9.30
CHEMBL119256 1 9.22
CHEMBL119116 1 9.22
CHEMBL119873 1 9.15
CHEMBL116981 1 9.05
CHEMBL115970 1 9.05
CHEMBL118815 1 8.92
CHEMBL332667 1 8.89
CHEMBL332373 1 8.82
CHEMBL118508 1 8.72
CHEMBL432813 1 8.64
CHEMBL117403 1 8.64
CHEMBL117715 1 8.62
CHEMBL324820 1 8.60
CHEMBL117723 1 8.39
CHEMBL325247 1 8.14
CHEMBL118783 1 7.89
CHEMBL119239 1 7.85
CHEMBL117007 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118860 IC50 = 0.2 nM 9.70
CHEMBL119413 IC50 = 0.3 nM 9.52
CHEMBL333335 IC50 = 0.3 nM 9.52
CHEMBL441826 IC50 = 0.4 nM 9.40
CHEMBL119354 IC50 = 0.4 nM 9.40
CHEMBL119440 IC50 = 0.4 nM 9.40
CHEMBL119382 IC50 = 0.5 nM 9.30
CHEMBL331054 IC50 = 0.5 nM 9.30
CHEMBL323617 IC50 = 0.5 nM 9.30
CHEMBL119256 IC50 = 0.6 nM 9.22
CHEMBL119116 IC50 = 0.6 nM 9.22
CHEMBL119873 IC50 = 0.7 nM 9.15
CHEMBL116981 IC50 = 0.9 nM 9.05
CHEMBL115970 IC50 = 0.9 nM 9.05
CHEMBL118815 IC50 = 1.2 nM 8.92
CHEMBL332667 IC50 = 1.3 nM 8.89
CHEMBL332373 IC50 = 1.5 nM 8.82
CHEMBL118508 IC50 = 1.9 nM 8.72
CHEMBL432813 IC50 = 2.3 nM 8.64
CHEMBL117403 IC50 = 2.3 nM 8.64
CHEMBL117715 IC50 = 2.4 nM 8.62
CHEMBL324820 IC50 = 2.5 nM 8.60
CHEMBL117723 IC50 = 4.1 nM 8.39
CHEMBL325247 IC50 = 7.3 nM 8.14
CHEMBL118783 IC50 = 13.0 nM 7.89
CHEMBL119239 IC50 = 14.0 nM 7.85
CHEMBL117007 IC50 = 32.0 nM 7.50