Assay Detail
ADMET
CHEMBL1022738
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AUC (0 to 4 hrs) in mouse plasma at 20 mg/kg, po
24
Total Activities
24
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Mus musculus |
| Tissue | Plasma |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.47 | 9.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| DOSE | DOSE | 20.0 | mg.kg-1 | — |
| ROUTE | ROUTE | - | — | Oral |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL519300 | — | — | 1 | 9.70 |
| CHEMBL520419 | — | — | 1 | 9.30 |
| CHEMBL474469 | — | — | 1 | 9.30 |
| CHEMBL506169 | — | — | 1 | 9.22 |
| CHEMBL454515 | — | — | 1 | 8.96 |
| CHEMBL459118 | — | — | 1 | 8.96 |
| CHEMBL499584 | — | — | 1 | 8.85 |
| CHEMBL502778 | — | — | 1 | 8.59 |
| CHEMBL482126 | — | — | 1 | 8.48 |
| CHEMBL505652 | — | — | 1 | 8.41 |
| CHEMBL510298 | — | — | 1 | 8.35 |
| CHEMBL519132 | — | — | 1 | 8.35 |
| CHEMBL502092 | — | — | 1 | 8.16 |
| CHEMBL482089 | — | — | 1 | 8.16 |
| CHEMBL480966 | — | — | 1 | 8.13 |
| CHEMBL450610 | — | — | 1 | 7.99 |
| CHEMBL505919 | — | — | 1 | 7.95 |
| CHEMBL482101 | — | — | 1 | 7.73 |
| CHEMBL521271 | — | — | 1 | 7.54 |
| CHEMBL401930 | — | — | 1 | 7.29 |
| CHEMBL482102 | — | — | 1 | - |
| CHEMBL480965 | — | — | 1 | - |
| CHEMBL454467 | — | — | 1 | - |
| CHEMBL451331 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL519300 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL520419 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL474469 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL506169 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL454515 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL459118 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL499584 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL502778 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL482126 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL505652 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL510298 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL519132 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL502092 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL482089 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL480966 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL450610 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL505919 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL482101 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL521271 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL401930 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL482102 | — | IC50 | = | - | nM | - |
| CHEMBL480965 | — | IC50 | = | - | nM | - |
| CHEMBL454467 | — | IC50 | = | - | nM | - |
| CHEMBL451331 | — | IC50 | = | - | nM | - |