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

CHEMBL2050358

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

Binding
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])-phenylmethoxy]biphenyl-3-yl}methoxy)phenyl]propanoic acid from rat GPR40 expressed in CHO cells after 90 mins by liquid scintillation counting in the presence of 0.2%BSA
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Free fatty acid receptor 1 (CHEMBL1795180)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 23 6.66 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047164 1 7.25
CHEMBL2047170 1 7.23
CHEMBL2047161 1 7.18
CHEMBL2047151 1 7.08
CHEMBL2047169 1 6.96
CHEMBL2047152 1 6.96
CHEMBL2047166 1 6.92
CHEMBL2047159 1 6.85
CHEMBL2047155 1 6.77
CHEMBL2047160 1 6.77
CHEMBL2047158 1 6.77
CHEMBL2047157 1 6.77
CHEMBL2047163 1 6.72
CHEMBL2047168 1 6.70
CHEMBL2047154 1 6.68
CHEMBL2047149 1 6.62
CHEMBL2047167 1 6.57
CHEMBL2022577 1 6.52
CHEMBL2047162 1 6.44
CHEMBL2047165 1 6.40
CHEMBL2047156 1 6.29
CHEMBL2047153 1 5.66
CHEMBL2047150 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047164 Ki = 56.0 nM 7.25
CHEMBL2047170 Ki = 59.0 nM 7.23
CHEMBL2047161 Ki = 66.0 nM 7.18
CHEMBL2047151 Ki = 83.0 nM 7.08
CHEMBL2047169 Ki = 110.0 nM 6.96
CHEMBL2047152 Ki = 110.0 nM 6.96
CHEMBL2047166 Ki = 120.0 nM 6.92
CHEMBL2047159 Ki = 140.0 nM 6.85
CHEMBL2047155 Ki = 170.0 nM 6.77
CHEMBL2047160 Ki = 170.0 nM 6.77
CHEMBL2047158 Ki = 170.0 nM 6.77
CHEMBL2047157 Ki = 170.0 nM 6.77
CHEMBL2047163 Ki = 190.0 nM 6.72
CHEMBL2047168 Ki = 200.0 nM 6.70
CHEMBL2047154 Ki = 210.0 nM 6.68
CHEMBL2047149 Ki = 240.0 nM 6.62
CHEMBL2047167 Ki = 270.0 nM 6.57
CHEMBL2022577 Ki = 300.0 nM 6.52
CHEMBL2047162 Ki = 360.0 nM 6.44
CHEMBL2047165 Ki = 400.0 nM 6.40
CHEMBL2047156 Ki = 510.0 nM 6.29
CHEMBL2047153 Ki = 2200.0 nM 5.66
CHEMBL2047150 Ki = 7400.0 nM 5.13