Assay Detail
Binding
CHEMBL4766270
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-TAK-875 from human recombinant full-length GPR40 expressed in human HEK293 cell membrane incubated for 2 hrs by solid scintillation counting method
34
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | 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 |
|---|---|---|---|
| Ki | 31 | 7.90 | 8.96 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787010 | — | — | 1 | 8.96 |
| CHEMBL4793371 | — | — | 1 | 8.89 |
| CHEMBL4797858 | — | — | 1 | 8.82 |
| CHEMBL4798993 | — | — | 1 | 8.82 |
| CHEMBL1829173 | — | — | 1 | 8.66 |
| CHEMBL4781604 | — | — | 1 | 8.60 |
| CHEMBL4788206 | — | — | 1 | 8.57 |
| CHEMBL4785057 | — | — | 1 | 8.46 |
| CHEMBL4797124 | — | — | 1 | 8.46 |
| CHEMBL4798023 | — | — | 1 | 8.40 |
| CHEMBL4800563 | — | — | 1 | 8.39 |
| CHEMBL4791842 | — | — | 1 | 8.34 |
| CHEMBL3915620 | LY2881835 | 1.0 | 2 | 8.33 |
| CHEMBL4782004 | — | — | 1 | 8.32 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 8.11 |
| CHEMBL4787498 | — | — | 2 | 8.09 |
| CHEMBL4780641 | — | — | 1 | 7.96 |
| CHEMBL4787628 | — | — | 1 | 7.89 |
| CHEMBL4786335 | — | — | 1 | 7.85 |
| CHEMBL4799453 | — | — | 1 | 7.80 |
| CHEMBL4792075 | — | — | 1 | 7.70 |
| CHEMBL4784555 | — | — | 1 | 7.54 |
| CHEMBL4783033 | — | — | 1 | 7.23 |
| CHEMBL4783190 | — | — | 1 | 7.17 |
| CHEMBL4778264 | — | — | 1 | 7.10 |
| CHEMBL4794233 | — | — | 1 | 7.00 |
| CHEMBL4790921 | — | — | 1 | 6.92 |
| CHEMBL4795763 | — | — | 1 | 6.89 |
| CHEMBL4794904 | — | — | 1 | 6.70 |
| CHEMBL4792027 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787010 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4793371 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4797858 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4798993 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1829173 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4781604 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4788206 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4785057 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL4797124 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL4798023 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4800563 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL4791842 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3915620 | LY2881835 | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL4782004 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL1829174 | FASIGLIFAM | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL4787498 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL4780641 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4787628 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4786335 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4799453 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4792075 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4784555 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4783033 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4783190 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4778264 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL4794233 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4790921 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4795763 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4794904 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL4792027 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4786299 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL3915620 | LY2881835 | Activity | - | — | - | |
| CHEMBL4787498 | — | Activity | - | — | - | |
| CHEMBL3955132 | — | Activity | - | — | - |