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Assay Detail

CHEMBL1960544

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Functional
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 1 (CHEMBL1914263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Nara F, Kawase Y, Yabe Y, Nakai D, Kamiyama E, Urasaki-Kaneno Y, Shimozato T, Doi-Komuro H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Nishi T.
Eur J Med Chem (2012) 51 : 92 -98
PubMed 22405291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 9.03 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366208 FTY720-P -1.0 1 9.54
CHEMBL1951304 1 8.82
CHEMBL1951588 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366208 FTY720-P EC50 = 0.29 nM 9.54
CHEMBL1951304 EC50 = 1.5 nM 8.82
CHEMBL1951588 EC50 = 1.8 nM 8.74