Assay Detail
Binding
CHEMBL1102236
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant IGF-1R tyrosine kinase expressed in baculovirus system assessed as [33gamma]ATP phosphorylation of poly(Glu/Tyr) substrate after 45 mins by scintillation counting
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.77 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1097358 | — | — | 1 | 7.75 |
| CHEMBL1077339 | — | — | 1 | 7.54 |
| CHEMBL1078891 | — | — | 1 | 7.50 |
| CHEMBL1097357 | — | — | 1 | 7.50 |
| CHEMBL256072 | — | — | 1 | 7.42 |
| CHEMBL1078991 | — | — | 1 | 7.38 |
| CHEMBL482126 | — | — | 1 | 7.35 |
| CHEMBL480966 | — | — | 1 | 7.30 |
| CHEMBL256908 | — | — | 1 | 7.17 |
| CHEMBL1078892 | — | — | 1 | 7.15 |
| CHEMBL482101 | — | — | 1 | 7.12 |
| CHEMBL256074 | — | — | 1 | 7.12 |
| CHEMBL505919 | — | — | 1 | 7.09 |
| CHEMBL256073 | — | — | 1 | 7.08 |
| CHEMBL256909 | — | — | 1 | 7.04 |
| CHEMBL401930 | — | — | 1 | 7.00 |
| CHEMBL256703 | — | — | 1 | 6.96 |
| CHEMBL401766 | — | — | 1 | 6.92 |
| CHEMBL256702 | — | — | 1 | 6.80 |
| CHEMBL256275 | — | — | 1 | 6.72 |
| CHEMBL256494 | — | — | 1 | 6.54 |
| CHEMBL1077324 | — | — | 1 | 6.48 |
| CHEMBL256910 | — | — | 1 | 6.48 |
| CHEMBL256277 | — | — | 1 | 6.44 |
| CHEMBL404307 | — | — | 1 | 6.44 |
| CHEMBL1077325 | — | — | 1 | 6.39 |
| CHEMBL256276 | — | — | 1 | 6.32 |
| CHEMBL403218 | — | — | 1 | 6.26 |
| CHEMBL404308 | — | — | 1 | 6.17 |
| CHEMBL1090744 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1097358 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1077339 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1078891 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1097357 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL256072 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1078991 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL482126 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL480966 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL256908 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1078892 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL482101 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL256074 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL505919 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL256073 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL256909 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL401930 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL256703 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL401766 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL256702 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL256275 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL256494 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1077324 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL256910 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL256277 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL404307 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1077325 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL256276 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL403218 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL404308 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1090744 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1091483 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1091820 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL1093748 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL1088741 | — | IC50 | = | 5210.0 | nM | 5.28 |