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Assay Detail

CHEMBL1110630

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Functional
Agonist activity at human S1P3 receptor assessed as effect on calcium mobilization by Gi dependent whole cell assay
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Ma B, Guckian KM, Lin EY, Lee WC, Scott D, Kumaravel G, Macdonald TL, Lynch KR, Black C, Chollate S, Hahm K, Hetu G, Jin P, Luo Y, Rohde E, Rossomando A, Scannevin R, Wang J, Yang C.
Bioorg Med Chem Lett (2010) 20 : 2264 -2269
PubMed 20188554 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 9.65 9.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366208 FTY720-P -1.0 1 9.87
CHEMBL1089004 1 9.82
CHEMBL1091103 2 9.67
CHEMBL1093686 1 9.54
CHEMBL225155 1 9.35
CHEMBL190006 1 -
CHEMBL1089005 1 -
CHEMBL1090758 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366208 FTY720-P EC50 = 0.134 nM 9.87
CHEMBL1089004 EC50 = 0.15 nM 9.82
CHEMBL1091103 EC50 = 0.215 nM 9.67
CHEMBL1093686 EC50 = 0.286 nM 9.54
CHEMBL225155 EC50 = 0.449 nM 9.35
CHEMBL190006 EC50 > 5000.0 nM -
CHEMBL1091103 EC50 > 5000.0 nM -
CHEMBL1089005 EC50 > 5000.0 nM -
CHEMBL1090758 EC50 > 5000.0 nM -