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Assay Detail

CHEMBL2051552

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 human GPR40 receptor expressed in CHO cell membrane after 90 mins by liquid scintillation counting in the presence of 0.2% BSA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 phenylpropanoic acid derivatives containing polar functionalities as potent and orally bioavailable G protein-coupled receptor 40 agonists for the treatment of type 2 diabetes.
Mikami S, Kitamura S, Negoro N, Sasaki S, Suzuki M, Tsujihata Y, Miyazaki T, Ito R, Suzuki N, Miyazaki J, Santou T, Kanzaki N, Funami M, Tanaka T, Yasuma T, Momose Y.
J Med Chem (2012) 55 : 3756 -3776
PubMed 22428944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.57 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2048620 1 7.92
CHEMBL2048618 1 7.92
CHEMBL2048616 1 7.82
CHEMBL2048622 1 7.82
CHEMBL2048615 1 7.80
CHEMBL2048623 1 7.80
CHEMBL2048628 1 7.75
CHEMBL2048626 1 7.75
CHEMBL2048627 1 7.72
CHEMBL2048624 1 7.72
CHEMBL2048625 1 7.70
CHEMBL2048619 1 7.70
CHEMBL2048621 1 7.68
CHEMBL2048617 1 7.64
CHEMBL2048614 1 7.60
CHEMBL1688473 1 7.50
CHEMBL1688486 1 7.34
CHEMBL2048613 1 7.33
CHEMBL2048610 1 7.24
CHEMBL2048612 1 7.00
CHEMBL2048611 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2048620 Ki = 12.0 nM 7.92
CHEMBL2048618 Ki = 12.0 nM 7.92
CHEMBL2048616 Ki = 15.0 nM 7.82
CHEMBL2048622 Ki = 15.0 nM 7.82
CHEMBL2048615 Ki = 16.0 nM 7.80
CHEMBL2048623 Ki = 16.0 nM 7.80
CHEMBL2048628 Ki = 18.0 nM 7.75
CHEMBL2048626 Ki = 18.0 nM 7.75
CHEMBL2048627 Ki = 19.0 nM 7.72
CHEMBL2048624 Ki = 19.0 nM 7.72
CHEMBL2048625 Ki = 20.0 nM 7.70
CHEMBL2048619 Ki = 20.0 nM 7.70
CHEMBL2048621 Ki = 21.0 nM 7.68
CHEMBL2048617 Ki = 23.0 nM 7.64
CHEMBL2048614 Ki = 25.0 nM 7.60
CHEMBL1688473 Ki = 32.0 nM 7.50
CHEMBL1688486 Ki = 46.0 nM 7.34
CHEMBL2048613 Ki = 47.0 nM 7.33
CHEMBL2048610 Ki = 58.0 nM 7.24
CHEMBL2048612 Ki = 99.0 nM 7.00
CHEMBL2048611 Ki = 520.0 nM 6.28