Assay Detail
Binding
CHEMBL2051553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3-[4-({2',6'-dimethyl-6-[(4-[3H])phenylmethoxy]biphenyl-3-yl}methoxy)phenyl] propanoic acid from rat 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 | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.84 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2048622 | — | — | 1 | 8.38 |
| CHEMBL2048625 | — | — | 1 | 8.35 |
| CHEMBL2048627 | — | — | 1 | 8.35 |
| CHEMBL2048618 | — | — | 1 | 8.35 |
| CHEMBL2048626 | — | — | 1 | 8.29 |
| CHEMBL2048615 | — | — | 1 | 8.25 |
| CHEMBL2048628 | — | — | 1 | 8.21 |
| CHEMBL2048614 | — | — | 1 | 8.21 |
| CHEMBL2048623 | — | — | 1 | 8.19 |
| CHEMBL2048619 | — | — | 1 | 8.17 |
| CHEMBL2048620 | — | — | 1 | 8.17 |
| CHEMBL2048616 | — | — | 1 | 8.17 |
| CHEMBL2048624 | — | — | 1 | 8.09 |
| CHEMBL2048621 | — | — | 1 | 8.01 |
| CHEMBL2048617 | — | — | 1 | 8.00 |
| CHEMBL1688486 | — | — | 1 | 7.57 |
| CHEMBL2048610 | — | — | 1 | 7.52 |
| CHEMBL1688473 | — | — | 1 | 7.44 |
| CHEMBL2048613 | — | — | 1 | 7.06 |
| CHEMBL2048612 | — | — | 1 | 6.92 |
| CHEMBL2048611 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2048622 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL2048625 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2048627 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2048618 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2048626 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL2048615 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL2048628 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2048614 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2048623 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL2048619 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2048620 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2048616 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2048624 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL2048621 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL2048617 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1688486 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL2048610 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1688473 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL2048613 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL2048612 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2048611 | — | Ki | = | 10000.0 | nM | 5.00 |