Assay Detail
ADMET
CHEMBL887758
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Inhibition of CYP1A2 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 | 5.12 | 7.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL397667 | — | — | 1 | 7.28 |
| CHEMBL230309 | — | — | 1 | 6.42 |
| CHEMBL230205 | — | — | 1 | 6.24 |
| CHEMBL230308 | — | — | 1 | 5.50 |
| CHEMBL231620 | — | — | 1 | 5.24 |
| CHEMBL231609 | — | — | 1 | 5.01 |
| CHEMBL390002 | — | — | 1 | 5.00 |
| CHEMBL230042 | — | — | 1 | 4.96 |
| CHEMBL440964 | — | — | 1 | 4.92 |
| CHEMBL231509 | — | — | 1 | 4.82 |
| CHEMBL230043 | — | — | 1 | 4.70 |
| CHEMBL231409 | — | — | 1 | 4.68 |
| CHEMBL425819 | — | — | 1 | 4.60 |
| CHEMBL387611 | — | — | 1 | 4.28 |
| CHEMBL231610 | — | — | 1 | 4.23 |
| CHEMBL231510 | — | — | 1 | 4.03 |
| CHEMBL230412 | — | — | 1 | - |
| CHEMBL397666 | — | — | 1 | - |
| CHEMBL231306 | — | — | 1 | - |
| CHEMBL230204 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL397667 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL230309 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL230205 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL230308 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL231620 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL231609 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL390002 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL230042 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL440964 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL231509 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL230043 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL231409 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL425819 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL387611 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL231610 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL231510 | — | IC50 | = | 93000.0 | nM | 4.03 |
| CHEMBL230412 | — | IC50 | - | — | - | |
| CHEMBL397666 | — | IC50 | < | 30.0 | nM | - |
| CHEMBL231306 | — | IC50 | < | 40.0 | nM | - |
| CHEMBL230204 | — | IC50 | < | 40.0 | nM | - |