Assay Detail
Binding
CHEMBL5098671
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Inhibition of CDK9 (unknown origin) using FITC-X-GSRTPMY-NH2 as substrate preincubated for 10 mins followed by substrate addition and measured after 90 mins in the presence of ATP at Km concentration by plate reader 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
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.64 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5173041 | — | — | 1 | 8.05 |
| CHEMBL5207813 | — | — | 1 | 8.00 |
| CHEMBL5188442 | — | — | 1 | 7.72 |
| CHEMBL5201044 | — | — | 1 | 7.47 |
| CHEMBL5191333 | — | — | 1 | 7.33 |
| CHEMBL5192139 | — | — | 1 | 7.24 |
| CHEMBL5170195 | — | — | 1 | - |
| CHEMBL3663760 | — | — | 1 | - |
| CHEMBL5170524 | — | — | 1 | - |
| CHEMBL5197170 | — | — | 1 | - |
| CHEMBL5198038 | — | — | 1 | - |
| CHEMBL5207871 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5173041 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5207813 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5188442 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5201044 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5191333 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5192139 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5170195 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL3663760 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5170524 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5197170 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5198038 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL5207871 | — | IC50 | < | 3.0 | nM | - |