Assay Detail
Binding
CHEMBL5376175
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Inhibition of human CDK9/Cyclin T1 preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs
39
Total Activities
39
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
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.17 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5440829 | — | — | 1 | 8.40 |
| CHEMBL5199065 | ISTISOCICLIB | 2.0 | 1 | 8.22 |
| CHEMBL5420915 | — | — | 1 | 8.22 |
| CHEMBL5428866 | — | — | 1 | 8.05 |
| CHEMBL5440226 | — | — | 1 | 8.00 |
| CHEMBL5419715 | — | — | 1 | 8.00 |
| CHEMBL5438063 | — | — | 1 | 7.92 |
| CHEMBL5421527 | — | — | 1 | 7.85 |
| CHEMBL5409780 | — | — | 1 | 7.70 |
| CHEMBL5396123 | — | — | 1 | 7.68 |
| CHEMBL5419691 | — | — | 1 | 7.60 |
| CHEMBL5423100 | — | — | 1 | 7.60 |
| CHEMBL5411270 | — | — | 1 | 7.40 |
| CHEMBL5413258 | — | — | 1 | 7.37 |
| CHEMBL5409162 | — | — | 1 | 7.34 |
| CHEMBL5421587 | — | — | 1 | 7.33 |
| CHEMBL5440331 | — | — | 1 | 7.30 |
| CHEMBL5430225 | — | — | 1 | 7.26 |
| CHEMBL5419772 | — | — | 1 | 7.13 |
| CHEMBL5404877 | — | — | 1 | 7.10 |
| CHEMBL5439995 | — | — | 1 | 7.09 |
| CHEMBL5406720 | — | — | 1 | 7.04 |
| CHEMBL5405502 | — | — | 1 | 7.04 |
| CHEMBL5436706 | — | — | 1 | 7.02 |
| CHEMBL5425977 | — | — | 1 | 6.98 |
| CHEMBL5403832 | — | — | 1 | 6.97 |
| CHEMBL5424203 | — | — | 1 | 6.93 |
| CHEMBL5424511 | — | — | 1 | 6.81 |
| CHEMBL5438393 | — | — | 1 | 6.75 |
| CHEMBL5438750 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5440829 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5199065 | ISTISOCICLIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5420915 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5428866 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5440226 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5419715 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5438063 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5421527 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5409780 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5396123 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5423100 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5419691 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5411270 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5413258 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5409162 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL5421587 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5440331 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5430225 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5419772 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5404877 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5439995 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5406720 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5405502 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5436706 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5425977 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5403832 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5424203 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL5424511 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5438393 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5438750 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5421956 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL5398523 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL5416160 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL5395908 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL5395824 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL5411384 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL5414916 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL5413604 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5434011 | — | IC50 | = | 2815.0 | nM | 5.55 |