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Assay Detail

CHEMBL1111629

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Functional
Agonist activity at human S1P1 receptor expressed in human Chem1 cells assessed as intracellular calcium mobilization
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Chem1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate.
Hamada M, Nakamura M, Kiuchi M, Marukawa K, Tomatsu A, Shimano K, Sato N, Sugahara K, Asayama M, Takagi K, Adachi K.
J Med Chem (2010) 53 : 3154 -3168
PubMed 20337461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 8.79 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114606 1 9.46
CHEMBL1089557 1 9.28
CHEMBL1092577 1 9.21
CHEMBL1096210 1 9.19
CHEMBL1096211 1 9.09
CHEMBL1090819 1 9.08
CHEMBL1092272 1 8.96
CHEMBL1095889 1 8.96
CHEMBL1089558 1 8.92
CHEMBL1091630 1 8.89
CHEMBL1090223 1 8.80
CHEMBL1092284 1 8.74
CHEMBL1089809 1 8.70
CHEMBL1092285 1 8.68
CHEMBL1089475 1 8.52
CHEMBL1089564 1 8.51
CHEMBL1092286 1 8.44
CHEMBL1089810 1 8.38
CHEMBL1093574 1 8.33
CHEMBL1093573 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114606 EC50 = 0.35 nM 9.46
CHEMBL1089557 EC50 = 0.53 nM 9.28
CHEMBL1092577 EC50 = 0.62 nM 9.21
CHEMBL1096210 EC50 = 0.64 nM 9.19
CHEMBL1096211 EC50 = 0.81 nM 9.09
CHEMBL1090819 EC50 = 0.84 nM 9.08
CHEMBL1092272 EC50 = 1.1 nM 8.96
CHEMBL1095889 EC50 = 1.1 nM 8.96
CHEMBL1089558 EC50 = 1.2 nM 8.92
CHEMBL1091630 EC50 = 1.3 nM 8.89
CHEMBL1090223 EC50 = 1.6 nM 8.80
CHEMBL1092284 EC50 = 1.8 nM 8.74
CHEMBL1089809 EC50 = 2.0 nM 8.70
CHEMBL1092285 EC50 = 2.1 nM 8.68
CHEMBL1089475 EC50 = 3.0 nM 8.52
CHEMBL1089564 EC50 = 3.1 nM 8.51
CHEMBL1092286 EC50 = 3.6 nM 8.44
CHEMBL1089810 EC50 = 4.2 nM 8.38
CHEMBL1093574 EC50 = 4.7 nM 8.33
CHEMBL1093573 EC50 = 21.0 nM 7.68