Assay Detail
Binding
CHEMBL4323740
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Binding affinity to recombinant full length human CYP51 expressed in Escherichia coli incubated for 30 sec using [3H] labelled 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 |
|---|---|---|---|
| Kd | 12 | 6.45 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4461447 | — | — | 1 | 7.70 |
| CHEMBL4277680 | — | — | 1 | 7.22 |
| CHEMBL3629567 | — | — | 1 | 7.05 |
| CHEMBL4522116 | — | — | 1 | 7.05 |
| CHEMBL4439225 | — | — | 1 | 6.89 |
| CHEMBL4435160 | — | — | 1 | 6.82 |
| CHEMBL4444489 | — | — | 1 | 6.33 |
| CHEMBL4593688 | — | — | 1 | 5.94 |
| CHEMBL4458275 | — | — | 1 | 5.78 |
| CHEMBL4472919 | — | — | 1 | 5.63 |
| CHEMBL4466288 | — | — | 1 | 5.60 |
| CHEMBL4452294 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4461447 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL4277680 | — | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL3629567 | — | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL4522116 | — | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL4439225 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL4435160 | — | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL4444489 | — | Kd | = | 470.0 | nM | 6.33 |
| CHEMBL4593688 | — | Kd | = | 1150.0 | nM | 5.94 |
| CHEMBL4458275 | — | Kd | = | 1650.0 | nM | 5.78 |
| CHEMBL4472919 | — | Kd | = | 2320.0 | nM | 5.63 |
| CHEMBL4466288 | — | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL4452294 | — | Kd | = | 3900.0 | nM | 5.41 |