Assay Detail
Binding
CHEMBL1695282
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Inhibition of auto-phosphorylation of human IR expressed in human HepG2 cells after 2 hrs by luminometry
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.81 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1688361 | — | — | 1 | 7.32 |
| CHEMBL1688363 | — | — | 1 | 7.17 |
| CHEMBL1667935 | — | — | 1 | 7.12 |
| CHEMBL1688360 | — | — | 1 | 6.58 |
| CHEMBL1688362 | — | — | 1 | 6.50 |
| CHEMBL1688359 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1688361 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1688363 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1667935 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1688360 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1688362 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1688359 | — | IC50 | = | 700.0 | nM | 6.16 |