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Assay Detail

CHEMBL4032276

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Functional
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by ELISA
3
Total Activities
3
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 1 (CHEMBL4333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a 1-Methyl-3,4-dihydronaphthalene-Based Sphingosine-1-Phosphate (S1P) Receptor Agonist Ceralifimod (ONO-4641). A S1P1 and S1P5 Selective Agonist for the Treatment of Autoimmune Diseases.
Kurata H, Kusumi K, Otsuki K, Suzuki R, Kurono M, Komiya T, Hagiya H, Mizuno H, Shioya H, Ono T, Takada Y, Maeda T, Matsunaga N, Kondo T, Tominaga S, Nunoya KI, Kiyoshi H, Komeno M, Nakade S, Habashita H.
J Med Chem (2017) 60 : 9508 -9530
PubMed 29120624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 10.14 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093489 1 10.57
CHEMBL4095920 1 10.14
CHEMBL4087932 1 9.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093489 EC50 = 0.027 nM 10.57
CHEMBL4095920 EC50 = 0.072 nM 10.14
CHEMBL4087932 EC50 = 0.19 nM 9.72