Assay Detail
ADMET
CHEMBL3636901
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Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.13 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3632717 | — | — | 1 | 5.75 |
| CHEMBL3632721 | — | — | 1 | 5.48 |
| CHEMBL3632724 | — | — | 1 | 5.47 |
| CHEMBL3632718 | — | — | 1 | 5.15 |
| CHEMBL3632719 | — | — | 1 | 5.00 |
| CHEMBL3632723 | — | — | 1 | 4.58 |
| CHEMBL3632720 | — | — | 1 | 4.47 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | - |
| CHEMBL3632722 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3632717 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3632721 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3632724 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3632718 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3632719 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3632723 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3632720 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL558752 | RAF-265 | IC50 | > | 40000.0 | nM | - |
| CHEMBL3632722 | — | IC50 | > | 40000.0 | nM | - |