Assay Detail
Binding
CHEMBL4323745
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Inhibition of recombinant full length human CYP51 expressed in Escherichia coli incubated for 1 hr using [3H] lanosterol as substrate by HPLC analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.03 | 5.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439225 | — | — | 1 | 5.44 |
| CHEMBL4461447 | — | — | 1 | 5.36 |
| CHEMBL4277680 | — | — | 1 | 5.23 |
| CHEMBL4444489 | — | — | 1 | 4.82 |
| CHEMBL4466288 | — | — | 1 | 4.72 |
| CHEMBL3629567 | — | — | 1 | 4.61 |
| CHEMBL4458275 | — | — | 1 | - |
| CHEMBL4593688 | — | — | 1 | - |
| CHEMBL4452294 | — | — | 1 | - |
| CHEMBL4472919 | — | — | 1 | - |
| CHEMBL4435160 | — | — | 1 | - |
| CHEMBL4522116 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439225 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4461447 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4277680 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4444489 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4466288 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3629567 | — | IC50 | = | 24400.0 | nM | 4.61 |
| CHEMBL4458275 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4593688 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4452294 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4472919 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4435160 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4522116 | — | IC50 | < | 1000.0 | nM | - |