Assay Detail
Binding
CHEMBL5236940
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Inhibition of CDK9/Cyclin-T1 (unknown origin) assessed as reduction in substrate peptide phosphorylation using DYRKtide peptide as substrate preincubated for 12 mins followed by ATP addition and measured for 45 mins by mobility shift assay
23
Total Activities
22
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 PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.48 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5276905 | — | — | 1 | 8.21 |
| CHEMBL5281860 | — | — | 1 | 8.10 |
| CHEMBL5269336 | — | — | 1 | 8.10 |
| CHEMBL5280928 | — | — | 1 | 8.02 |
| CHEMBL5269912 | — | — | 1 | 7.82 |
| CHEMBL5287843 | — | — | 1 | 7.79 |
| CHEMBL5277190 | — | — | 2 | 7.74 |
| CHEMBL4446357 | EBVACICLIB | 2.0 | 1 | 7.71 |
| CHEMBL4752291 | — | — | 1 | 7.52 |
| CHEMBL5278622 | — | — | 1 | 7.50 |
| CHEMBL5271753 | — | — | 1 | 7.43 |
| CHEMBL5272948 | — | — | 1 | 7.41 |
| CHEMBL5271882 | — | — | 1 | 7.38 |
| CHEMBL4796501 | — | — | 1 | 7.27 |
| CHEMBL5283828 | — | — | 1 | 6.96 |
| CHEMBL5285163 | — | — | 1 | 6.88 |
| CHEMBL5278015 | — | — | 1 | 6.79 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 6.70 |
| CHEMBL5281770 | — | — | 1 | 6.67 |
| CHEMBL5275378 | — | — | 1 | - |
| CHEMBL5266837 | — | — | 1 | - |
| CHEMBL5288078 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5276905 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL5281860 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5269336 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5280928 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL5269912 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5287843 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL5277190 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL4446357 | EBVACICLIB | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL5277190 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL4752291 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL5278622 | — | Ki | = | 31.4 | nM | 7.50 |
| CHEMBL5271753 | — | Ki | = | 36.8 | nM | 7.43 |
| CHEMBL5272948 | — | Ki | = | 39.1 | nM | 7.41 |
| CHEMBL5271882 | — | Ki | = | 41.3 | nM | 7.38 |
| CHEMBL4796501 | — | Ki | = | 53.2 | nM | 7.27 |
| CHEMBL5283828 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL5285163 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL5278015 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL189963 | PALBOCICLIB | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL5281770 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL5275378 | — | Ki | > | 1200.0 | nM | - |
| CHEMBL5266837 | — | Ki | > | 1400.0 | nM | - |
| CHEMBL5288078 | — | Ki | > | 1200.0 | nM | - |