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Assay Detail

CHEMBL980648

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

Binding
Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Satz AL, Bernier SG, Kavarana MJ, Doyle E, Lorusso J, Taghizadeh N, Halley K, Hutchings A, Kelley MS, Wright AD, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett (2009) 19 : 2315 -2319
PubMed 19282175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.33 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470511 1 9.70
CHEMBL473156 1 9.68
CHEMBL516380 1 9.11
CHEMBL474407 1 9.08
CHEMBL515917 1 9.05
CHEMBL473238 1 9.05
CHEMBL514170 1 8.99
CHEMBL475405 1 8.98
CHEMBL473562 1 8.92
CHEMBL514302 1 8.68
CHEMBL473563 1 8.60
CHEMBL516035 1 8.32
CHEMBL475253 1 8.16
CHEMBL474418 1 8.11
CHEMBL475247 1 7.92
CHEMBL473016 1 7.68
CHEMBL473360 1 7.52
CHEMBL515603 1 6.73
CHEMBL514189 1 6.66
CHEMBL473237 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470511 IC50 = 0.2 nM 9.70
CHEMBL473156 IC50 = 0.21 nM 9.68
CHEMBL516380 IC50 = 0.78 nM 9.11
CHEMBL474407 IC50 = 0.84 nM 9.08
CHEMBL515917 IC50 = 0.9 nM 9.05
CHEMBL473238 IC50 = 0.9 nM 9.05
CHEMBL514170 IC50 = 1.03 nM 8.99
CHEMBL475405 IC50 = 1.05 nM 8.98
CHEMBL473562 IC50 = 1.2 nM 8.92
CHEMBL514302 IC50 = 2.1 nM 8.68
CHEMBL473563 IC50 = 2.5 nM 8.60
CHEMBL516035 IC50 = 4.75 nM 8.32
CHEMBL475253 IC50 = 6.9 nM 8.16
CHEMBL474418 IC50 = 7.7 nM 8.11
CHEMBL475247 IC50 = 12.0 nM 7.92
CHEMBL473016 IC50 = 21.0 nM 7.68
CHEMBL473360 IC50 = 30.0 nM 7.52
CHEMBL515603 IC50 = 186.0 nM 6.73
CHEMBL514189 IC50 = 220.0 nM 6.66
CHEMBL473237 IC50 = 2000.0 nM 5.70