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Assay Detail

CHEMBL3743673

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Functional
Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay
2
Total Activities
2
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 5 (CHEMBL2274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G, Kim Y, Larson K, Maull JW, Moore NS, Shi D, Shrestha A, Tang X, Zhang P, Sarris KK.
J Med Chem (2015) 58 : 9154 -9170
PubMed 26509640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.18 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3741589 1 8.39
CHEMBL114606 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3741589 EC50 = 4.1 nM 8.39
CHEMBL114606 EC50 = 11.0 nM 7.96