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Assay Detail

CHEMBL2155123

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 0.1 % human serum
23
Total Activities
23
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 23 5.93 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829173 1 7.22
CHEMBL2152070 1 6.80
CHEMBL2151298 1 6.43
CHEMBL2151299 1 6.38
CHEMBL2152069 1 6.32
CHEMBL2151288 1 6.19
CHEMBL2151295 1 6.17
CHEMBL2151296 1 6.16
CHEMBL2151294 1 6.11
CHEMBL2151293 1 6.05
CHEMBL2152071 1 5.96
CHEMBL2151292 1 5.92
CHEMBL2151302 1 5.92
CHEMBL2151300 1 5.88
CHEMBL2151291 1 5.72
CHEMBL2151301 1 5.68
CHEMBL2152068 1 5.68
CHEMBL2151297 1 5.66
CHEMBL2151290 1 5.64
CHEMBL2151287 1 5.64
CHEMBL2151289 1 5.40
CHEMBL1939651 1 5.11
CHEMBL367149 DOCONEXENT 3.0 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829173 EC50 = 60.0 nM 7.22
CHEMBL2152070 EC50 = 160.0 nM 6.80
CHEMBL2151298 EC50 = 370.0 nM 6.43
CHEMBL2151299 EC50 = 420.0 nM 6.38
CHEMBL2152069 EC50 = 480.0 nM 6.32
CHEMBL2151288 EC50 = 650.0 nM 6.19
CHEMBL2151295 EC50 = 680.0 nM 6.17
CHEMBL2151296 EC50 = 690.0 nM 6.16
CHEMBL2151294 EC50 = 770.0 nM 6.11
CHEMBL2151293 EC50 = 900.0 nM 6.05
CHEMBL2152071 EC50 = 1100.0 nM 5.96
CHEMBL2151292 EC50 = 1200.0 nM 5.92
CHEMBL2151302 EC50 = 1200.0 nM 5.92
CHEMBL2151300 EC50 = 1310.0 nM 5.88
CHEMBL2151291 EC50 = 1900.0 nM 5.72
CHEMBL2151301 EC50 = 2100.0 nM 5.68
CHEMBL2152068 EC50 = 2100.0 nM 5.68
CHEMBL2151297 EC50 = 2200.0 nM 5.66
CHEMBL2151290 EC50 = 2300.0 nM 5.64
CHEMBL2151287 EC50 = 2300.0 nM 5.64
CHEMBL2151289 EC50 = 4000.0 nM 5.40
CHEMBL1939651 EC50 = 7700.0 nM 5.11
CHEMBL367149 DOCONEXENT EC50 = 36000.0 nM 4.44