Assay Detail
ADMET
CHEMBL887697
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Inhibition of CYP3A4 in microsomes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Subcellular | Microsomes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.52 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230204 | — | — | 1 | 7.22 |
| CHEMBL397666 | — | — | 1 | 7.10 |
| CHEMBL231620 | — | — | 1 | 6.44 |
| CHEMBL230309 | — | — | 1 | 6.15 |
| CHEMBL231609 | — | — | 1 | 5.80 |
| CHEMBL231509 | — | — | 1 | 5.66 |
| CHEMBL397667 | — | — | 1 | 5.51 |
| CHEMBL230205 | — | — | 1 | 5.44 |
| CHEMBL231409 | — | — | 1 | 5.43 |
| CHEMBL390002 | — | — | 1 | 5.37 |
| CHEMBL230308 | — | — | 1 | 5.20 |
| CHEMBL440964 | — | — | 1 | 5.17 |
| CHEMBL231510 | — | — | 1 | 5.00 |
| CHEMBL231610 | — | — | 1 | 4.96 |
| CHEMBL230042 | — | — | 1 | 4.89 |
| CHEMBL425819 | — | — | 1 | 4.82 |
| CHEMBL230043 | — | — | 1 | 4.80 |
| CHEMBL387611 | — | — | 1 | 4.46 |
| CHEMBL230412 | — | — | 1 | - |
| CHEMBL231306 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230204 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL397666 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL231620 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL230309 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL231609 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL231509 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL397667 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL230205 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL231409 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL390002 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL230308 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL440964 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL231510 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL231610 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL230042 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL425819 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL230043 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL387611 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL230412 | — | IC50 | - | — | - | |
| CHEMBL231306 | — | IC50 | < | 46.0 | nM | - |