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Assay Detail

CHEMBL2155124

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

Functional
Agonist activity at GPR40 expressed in CHO cells after 20 seconds by aequorin bioluminescence assay in presence of 100 % human serum
4
Total Activities
4
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

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Brown SP, Dransfield PJ, Vimolratana M, Jiao X, Zhu L, Pattaropong V, Sun Y, Liu J, Luo J, Zhang J, Wong S, Zhuang R, Guo Q, Li F, Medina JC, Swaminath G, Lin DC, Houze JB.
ACS Med Chem Lett (2012) 3 : 726 -730
PubMed 24900539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.19 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152070 1 6.15
CHEMBL2151298 1 5.72
CHEMBL2152071 1 4.47
CHEMBL2152069 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152070 EC50 = 710.0 nM 6.15
CHEMBL2151298 EC50 = 1900.0 nM 5.72
CHEMBL2152071 EC50 = 34000.0 nM 4.47
CHEMBL2152069 EC50 = 38000.0 nM 4.42