Assay Detail
Binding
CHEMBL4766273
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant full-length Prolink-tagged GPR40 fused with EA-tagged beta-arrestin expressed in human HEK293 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| EC50 | 32 | 7.62 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787010 | — | — | 1 | 8.96 |
| CHEMBL4797858 | — | — | 1 | 8.82 |
| CHEMBL4793371 | — | — | 1 | 8.77 |
| CHEMBL4788206 | — | — | 1 | 8.54 |
| CHEMBL4785057 | — | — | 1 | 8.48 |
| CHEMBL4798993 | — | — | 1 | 8.48 |
| CHEMBL4797124 | — | — | 1 | 8.41 |
| CHEMBL4782004 | — | — | 1 | 8.28 |
| CHEMBL3955132 | — | — | 1 | 8.15 |
| CHEMBL4787498 | — | — | 1 | 8.10 |
| CHEMBL4800563 | — | — | 1 | 8.09 |
| CHEMBL3915620 | LY2881835 | 1.0 | 1 | 8.06 |
| CHEMBL4798023 | — | — | 1 | 8.03 |
| CHEMBL4781604 | — | — | 1 | 8.00 |
| CHEMBL4791842 | — | — | 1 | 7.96 |
| CHEMBL1829173 | — | — | 1 | 7.96 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.92 |
| CHEMBL4786335 | — | — | 1 | 7.60 |
| CHEMBL4799453 | — | — | 1 | 7.58 |
| CHEMBL4787628 | — | — | 1 | 7.44 |
| CHEMBL4780641 | — | — | 1 | 7.25 |
| CHEMBL4783033 | — | — | 1 | 7.24 |
| CHEMBL4792075 | — | — | 1 | 7.21 |
| CHEMBL4795763 | — | — | 1 | 7.08 |
| CHEMBL4784555 | — | — | 1 | 7.00 |
| CHEMBL4790921 | — | — | 1 | 6.77 |
| CHEMBL4783190 | — | — | 1 | 6.47 |
| CHEMBL4794233 | — | — | 1 | 6.28 |
| CHEMBL4792027 | — | — | 1 | 6.27 |
| CHEMBL4778264 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787010 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4797858 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4793371 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4788206 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4785057 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4798993 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4797124 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4782004 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3955132 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4787498 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4800563 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3915620 | LY2881835 | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4798023 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4781604 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1829173 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4791842 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4786335 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4799453 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4787628 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4780641 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4783033 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4792075 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4795763 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4784555 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4790921 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4783190 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4794233 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4792027 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4778264 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4786299 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4794904 | — | EC50 | = | 740.0 | nM | 6.13 |