Assay Detail
ADMET
CHEMBL4843795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human CYP3A4 expressed in Escherichia coli using VG as probe substrate incubated for 15 to 60 mins by fluorometric assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 4.90 | 5.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874801 | — | — | 1 | 5.10 |
| CHEMBL2017291 | — | — | 1 | 5.01 |
| CHEMBL4874356 | — | — | 1 | 5.00 |
| CHEMBL4874790 | — | — | 1 | 4.80 |
| CHEMBL4878439 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874801 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2017291 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4874356 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4874790 | — | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL4878439 | — | IC50 | = | 25100.0 | nM | 4.60 |