Assay Detail
Binding
CHEMBL3862053
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length human C-terminal His6-tagged CDK9/full-length human cyclin T1 expressed in baculovirus infected insect Sf21 cells using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate in presence of [gamma-33P]-ATP after 40 mins by scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.75 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3972065 | — | — | 1 | 8.10 |
| CHEMBL3928361 | — | — | 1 | 8.10 |
| CHEMBL3919811 | — | — | 1 | 7.85 |
| CHEMBL3919459 | — | — | 1 | 7.66 |
| CHEMBL3922414 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3972065 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3928361 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3919811 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3919459 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3922414 | — | IC50 | = | 88.0 | nM | 7.06 |