Assay Detail
ADMET
CHEMBL4843801
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Inhibition of recombinant human CYP2C9 expressed in Escherichia coli using FCA as substrate incubated for 15 to 60 mins by fluorometric assay
6
Total Activities
6
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 | 6 | 5.12 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874356 | — | — | 1 | 5.89 |
| CHEMBL4874801 | — | — | 1 | 5.10 |
| CHEMBL2017291 | — | — | 1 | 5.00 |
| CHEMBL4874790 | — | — | 1 | 4.50 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | - |
| CHEMBL4878439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874356 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4874801 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2017291 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4874790 | — | IC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | > | 50000.0 | nM | - |
| CHEMBL4878439 | — | IC50 | > | 50000.0 | nM | - |