Assay Detail
Binding
CHEMBL4377494
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Inhibition of recombinant full-length human CDK9/cyclinT1 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC peptide as substrate measured after 40 mins in presence of [gamma33P]ATP by scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.67 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4592737 | — | — | 1 | 8.22 |
| CHEMBL4573953 | — | — | 1 | 8.05 |
| CHEMBL4522831 | — | — | 1 | 8.05 |
| CHEMBL4463566 | — | — | 1 | 8.00 |
| CHEMBL4474633 | — | — | 1 | 7.96 |
| CHEMBL4548580 | — | — | 1 | 7.96 |
| CHEMBL4434746 | — | — | 1 | 7.92 |
| CHEMBL4569530 | — | — | 1 | 7.82 |
| CHEMBL4543127 | — | — | 1 | 7.60 |
| CHEMBL4556152 | — | — | 1 | 7.48 |
| CHEMBL4445923 | — | — | 1 | 7.47 |
| CHEMBL4466046 | — | — | 1 | 7.38 |
| CHEMBL4442345 | — | — | 1 | 7.30 |
| CHEMBL4468293 | — | — | 1 | 7.17 |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4592737 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4573953 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4522831 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4463566 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4474633 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4548580 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4434746 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4569530 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4543127 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4556152 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4445923 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4466046 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4442345 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4468293 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3545110 | RIBOCICLIB | IC50 | = | 197.0 | nM | 6.71 |