Assay Detail
Binding
CHEMBL5136675
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human CDK12/Cyclin K expressed in Sf9 cells using RBER-IRStide peptide as substrate in presence of ATP and [gamma33-P] ATP by radioisotope filter binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
3,5,7-Substituted Pyrazolo[4,3-<i>d</i>]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.24 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 8.15 |
| CHEMBL5169449 | — | — | 1 | 7.54 |
| CHEMBL5187378 | — | — | 1 | 7.30 |
| CHEMBL5194202 | — | — | 1 | 7.19 |
| CHEMBL5182767 | — | — | 1 | 7.14 |
| CHEMBL5191136 | — | — | 1 | 6.81 |
| CHEMBL5194833 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5169449 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5187378 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5194202 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5182767 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5191136 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5194833 | — | IC50 | = | 304.0 | nM | 6.52 |