Assay Detail
Functional
CHEMBL4766279
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant full length GPR40 overexpressed in human HEK293 cells assessed as increase in inositol phosphate accumulation in presence of terbium cryptate-labeled anti IP1/d2-labelled IP1 measured after 120 mins by HTRF assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 31 | 8.09 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1829174 | FASIGLIFAM | 3.0 | 1 | 9.46 |
| CHEMBL4782004 | — | — | 1 | 9.22 |
| CHEMBL4797124 | — | — | 1 | 9.01 |
| CHEMBL3915620 | LY2881835 | 1.0 | 1 | 8.92 |
| CHEMBL1829173 | — | — | 1 | 8.89 |
| CHEMBL4787010 | — | — | 1 | 8.72 |
| CHEMBL4797858 | — | — | 1 | 8.68 |
| CHEMBL4798023 | — | — | 1 | 8.64 |
| CHEMBL4786335 | — | — | 1 | 8.46 |
| CHEMBL4793371 | — | — | 1 | 8.38 |
| CHEMBL4788206 | — | — | 1 | 8.33 |
| CHEMBL4798993 | — | — | 1 | 8.31 |
| CHEMBL4790921 | — | — | 1 | 8.28 |
| CHEMBL4787498 | — | — | 1 | 8.21 |
| CHEMBL4791842 | — | — | 1 | 8.21 |
| CHEMBL4781604 | — | — | 1 | 8.13 |
| CHEMBL4799453 | — | — | 1 | 8.08 |
| CHEMBL4783033 | — | — | 1 | 8.00 |
| CHEMBL4800563 | — | — | 1 | 7.96 |
| CHEMBL4785057 | — | — | 1 | 7.96 |
| CHEMBL4795763 | — | — | 1 | 7.92 |
| CHEMBL4780641 | — | — | 1 | 7.92 |
| CHEMBL4787628 | — | — | 1 | 7.85 |
| CHEMBL4792075 | — | — | 1 | 7.66 |
| CHEMBL4784555 | — | — | 1 | 7.64 |
| CHEMBL4783190 | — | — | 1 | 7.41 |
| CHEMBL4778264 | — | — | 1 | 7.17 |
| CHEMBL4794233 | — | — | 1 | 7.14 |
| CHEMBL4794904 | — | — | 1 | 7.07 |
| CHEMBL4786299 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1829174 | FASIGLIFAM | EC50 | = | 0.35 | nM | 9.46 |
| CHEMBL4782004 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4797124 | — | EC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3915620 | LY2881835 | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1829173 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4787010 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4797858 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4798023 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4786335 | — | EC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4793371 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4788206 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4798993 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4790921 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4787498 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4791842 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4781604 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4799453 | — | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4783033 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4800563 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4785057 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4795763 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4780641 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4787628 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4792075 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4784555 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4783190 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4778264 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4794233 | — | EC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4794904 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4786299 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4792027 | — | EC50 | = | 360.0 | nM | 6.44 |