Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2050355

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

Functional
Agonist activity at human GP40 receptor expressed in CHO cells assessed as increase in intracellular calcium level for 90 secs by FLIPR assay in the presence of 0.1% BSA
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

Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.
Negoro N, Sasaki S, Mikami S, Ito M, Tsujihata Y, Ito R, Suzuki M, Takeuchi K, Suzuki N, Miyazaki J, Santou T, Odani T, Kanzaki N, Funami M, Morohashi A, Nonaka M, Matsunaga S, Yasuma T, Momose Y.
J Med Chem (2012) 55 : 3960 -3974
PubMed 22490067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 7.57 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047157 1 7.89
CHEMBL2047158 1 7.85
CHEMBL2047149 1 7.80
CHEMBL2047169 1 7.80
CHEMBL2047168 1 7.80
CHEMBL1829174 FASIGLIFAM 3.0 1 7.80
CHEMBL2047170 1 7.77
CHEMBL2047164 1 7.77
CHEMBL2047163 1 7.77
CHEMBL2047160 1 7.77
CHEMBL2047166 1 7.75
CHEMBL2047152 1 7.75
CHEMBL2047162 1 7.75
CHEMBL2047161 1 7.72
CHEMBL2047167 1 7.72
CHEMBL2047155 1 7.66
CHEMBL2047151 1 7.62
CHEMBL2047165 1 7.54
CHEMBL2022577 1 7.52
CHEMBL2047154 1 7.41
CHEMBL2047153 1 6.57
CHEMBL2047156 1 6.54
CHEMBL2047150 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047157 EC50 = 13.0 nM 7.89
CHEMBL2047158 EC50 = 14.0 nM 7.85
CHEMBL2047149 EC50 = 16.0 nM 7.80
CHEMBL2047169 EC50 = 16.0 nM 7.80
CHEMBL2047168 EC50 = 16.0 nM 7.80
CHEMBL1829174 FASIGLIFAM EC50 = 16.0 nM 7.80
CHEMBL2047170 EC50 = 17.0 nM 7.77
CHEMBL2047164 EC50 = 17.0 nM 7.77
CHEMBL2047163 EC50 = 17.0 nM 7.77
CHEMBL2047160 EC50 = 17.0 nM 7.77
CHEMBL2047166 EC50 = 18.0 nM 7.75
CHEMBL2047152 EC50 = 18.0 nM 7.75
CHEMBL2047162 EC50 = 18.0 nM 7.75
CHEMBL2047161 EC50 = 19.0 nM 7.72
CHEMBL2047167 EC50 = 19.0 nM 7.72
CHEMBL2047155 EC50 = 22.0 nM 7.66
CHEMBL2047151 EC50 = 24.0 nM 7.62
CHEMBL2047165 EC50 = 29.0 nM 7.54
CHEMBL2022577 EC50 = 30.0 nM 7.52
CHEMBL2047154 EC50 = 39.0 nM 7.41
CHEMBL2047153 EC50 = 270.0 nM 6.57
CHEMBL2047156 EC50 = 290.0 nM 6.54
CHEMBL2047150 EC50 = 290.0 nM 6.54