Assay Detail
ADMET
CHEMBL3540969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged CYP3A4 expressed in Escherichia coli TOPP3 using BFC as substrate after 15 mins by double reciprocal plot analysis in presence of NADPH and cytochrome b5
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 1 | 4.62 | 4.62 |
| Kinact | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1614710 | OSI-930 | 1.0 | 2 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1614710 | OSI-930 | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL1614710 | OSI-930 | Kinact | = | 0.04 | /min | - |