Assay Detail
Binding
CHEMBL4766277
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at Prolink-tagged rat GPR40 fused with EA-tagged beta-arrestin expressed in human U2OS 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 | Rattus norvegicus |
| Cell Type | U2OS |
| 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 | 8.12 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4793371 | — | — | 1 | 9.27 |
| CHEMBL4788206 | — | — | 1 | 9.23 |
| CHEMBL4797858 | — | — | 1 | 9.08 |
| CHEMBL4785057 | — | — | 1 | 9.05 |
| CHEMBL4782004 | — | — | 1 | 9.03 |
| CHEMBL4798993 | — | — | 1 | 9.00 |
| CHEMBL4797124 | — | — | 1 | 8.96 |
| CHEMBL4787010 | — | — | 1 | 8.96 |
| CHEMBL4798023 | — | — | 1 | 8.89 |
| CHEMBL4791842 | — | — | 1 | 8.89 |
| CHEMBL4787498 | — | — | 1 | 8.77 |
| CHEMBL3915620 | LY2881835 | 1.0 | 1 | 8.70 |
| CHEMBL4800563 | — | — | 1 | 8.68 |
| CHEMBL4781604 | — | — | 1 | 8.52 |
| CHEMBL3955132 | — | — | 1 | 8.52 |
| CHEMBL1829173 | — | — | 1 | 8.49 |
| CHEMBL4792075 | — | — | 1 | 8.38 |
| CHEMBL4799453 | — | — | 1 | 8.35 |
| CHEMBL4786335 | — | — | 1 | 8.34 |
| CHEMBL4780641 | — | — | 1 | 8.26 |
| CHEMBL4790921 | — | — | 1 | 7.96 |
| CHEMBL4787628 | — | — | 1 | 7.80 |
| CHEMBL4783033 | — | — | 1 | 7.77 |
| CHEMBL4784555 | — | — | 1 | 7.75 |
| CHEMBL4795763 | — | — | 1 | 7.64 |
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 7.44 |
| CHEMBL4794233 | — | — | 1 | 7.00 |
| CHEMBL4792027 | — | — | 1 | 6.92 |
| CHEMBL4783190 | — | — | 1 | 6.80 |
| CHEMBL4786299 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4793371 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4788206 | — | EC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4797858 | — | EC50 | = | 0.83 | nM | 9.08 |
| CHEMBL4785057 | — | EC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4782004 | — | EC50 | = | 0.93 | nM | 9.03 |
| CHEMBL4798993 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4797124 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4787010 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4798023 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4791842 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4787498 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3915620 | LY2881835 | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4800563 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4781604 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3955132 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1829173 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4792075 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4799453 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4786335 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4780641 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4790921 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4787628 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4783033 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4784555 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4795763 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4794233 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4792027 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4783190 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4786299 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4794904 | — | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4778264 | — | EC50 | = | 14000.0 | nM | 4.85 |