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Assay Detail

CHEMBL4184672

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

Functional
Agonist activity at human S1P3 receptor expressed in CHO cells assessed as increase in calcium flux by aequorin-derived luminescence assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Spiro-1-benzofuranpiperidinylalkanoic acids as a novel and selective sphingosine S1P5 receptor agonist chemotype.
Stoit AR, Lange JHM, Coolen HKAC, Rensink A, van den Hoogenband A, den Hartog AP, van Schaik S, Kruse CG.
Bioorg Med Chem Lett (2018) 28 : 459 -465
PubMed 29254642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 5.74 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205714 1 6.00
CHEMBL4204437 1 5.90
CHEMBL4207162 1 5.80
CHEMBL4203755 1 5.80
CHEMBL4205878 1 5.70
CHEMBL314854 FINGOLIMOD 4.0 1 5.60
CHEMBL4205124 1 5.40
CHEMBL4205748 1 -
CHEMBL4218296 1 -
CHEMBL4208771 1 -
CHEMBL4209307 1 -
CHEMBL4217349 1 -
CHEMBL4205225 1 -
CHEMBL4210019 1 -
CHEMBL4209494 1 -
CHEMBL4208055 1 -
CHEMBL4213894 1 -
CHEMBL4218826 1 -
CHEMBL4218094 1 -
CHEMBL4217573 1 -
CHEMBL4213167 1 -
CHEMBL4205333 1 -
CHEMBL4213649 1 -
CHEMBL4210234 1 -
CHEMBL4208787 1 -
CHEMBL4204779 1 -
CHEMBL4207361 1 -
CHEMBL4210576 1 -
CHEMBL4210080 1 -
CHEMBL4215002 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205714 EC50 = 1000.0 nM 6.00
CHEMBL4204437 EC50 = 1258.93 nM 5.90
CHEMBL4207162 EC50 = 1584.89 nM 5.80
CHEMBL4203755 EC50 = 1584.89 nM 5.80
CHEMBL4205878 EC50 = 1995.26 nM 5.70
CHEMBL314854 FINGOLIMOD EC50 = 2511.89 nM 5.60
CHEMBL4205124 EC50 = 3981.07 nM 5.40
CHEMBL4205748 EC50 > 10000.0 nM -
CHEMBL4206573 EC50 > 10000.0 nM -
CHEMBL4208771 EC50 > 10000.0 nM -
CHEMBL4209307 EC50 > 1000.0 nM -
CHEMBL4217349 EC50 > 10000.0 nM -
CHEMBL4205225 EC50 > 10000.0 nM -
CHEMBL4210019 EC50 > 1000.0 nM -
CHEMBL4209494 EC50 > 10000.0 nM -
CHEMBL4208055 EC50 > 10000.0 nM -
CHEMBL4213894 EC50 > 10000.0 nM -
CHEMBL4218826 EC50 > 10000.0 nM -
CHEMBL4218296 EC50 > 10000.0 nM -
CHEMBL4218094 EC50 > 10000.0 nM -
CHEMBL4217573 EC50 > 10000.0 nM -
CHEMBL4213167 EC50 > 10000.0 nM -
CHEMBL4205333 EC50 > 10000.0 nM -
CHEMBL4213649 EC50 > 10000.0 nM -
CHEMBL4210234 EC50 > 10000.0 nM -
CHEMBL4208787 EC50 > 10000.0 nM -
CHEMBL4204779 EC50 > 31622.78 nM -
CHEMBL4207361 EC50 > 10000.0 nM -
CHEMBL4210576 EC50 > 10000.0 nM -
CHEMBL4210080 EC50 > 10000.0 nM -
CHEMBL4215002 EC50 > 10000.0 nM -