Assay Detail
Binding
CHEMBL4766281
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(S)-2-(6-((2',6'-dimethyl-4'-(3-(methylsulfonyl)propoxy)biphenyl-3-yl)methoxy)-2,3-dihydrobenzofuran-3-yl)acetic acid from human recombinant full-length GPR40 expressed in human HEK293 cell membrane assessed as dissociation constant measured after 2 hrs by radioligand competitive assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 8.24 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1829173 | — | — | 1 | 8.72 |
| CHEMBL4782004 | — | — | 1 | 8.70 |
| CHEMBL4791842 | — | — | 1 | 8.66 |
| CHEMBL3915620 | LY2881835 | 1.0 | 1 | 8.60 |
| CHEMBL4787498 | — | — | 1 | 8.46 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 8.35 |
| CHEMBL4780641 | — | — | 1 | 8.02 |
| CHEMBL4778264 | — | — | 1 | 7.43 |
| CHEMBL4783190 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1829173 | — | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL4782004 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL4791842 | — | Kd | = | 2.2 | nM | 8.66 |
| CHEMBL3915620 | LY2881835 | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL4787498 | — | Kd | = | 3.5 | nM | 8.46 |
| CHEMBL1829174 | FASIGLIFAM | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL4780641 | — | Kd | = | 9.5 | nM | 8.02 |
| CHEMBL4778264 | — | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL4783190 | — | Kd | = | 58.0 | nM | 7.24 |