Assay Detail
Binding
CHEMBL5582249
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK9 (unknown origin) using ULight 4EBP1 peptide as substrate incubated for 2 hrs by FRET assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Biological Evaluation of 2,4-Diaminopyrimidine Derivatives as Potent CDK7 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.28 | 8.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3656841 | — | — | 1 | 8.45 |
| CHEMBL4754493 | BTX-A51 | 1.0 | 1 | 7.73 |
| CHEMBL5590934 | — | — | 1 | 7.41 |
| CHEMBL5593193 | — | — | 1 | 7.03 |
| CHEMBL5595728 | — | — | 1 | 6.86 |
| CHEMBL5593612 | — | — | 1 | 6.85 |
| CHEMBL5592046 | — | — | 1 | 6.78 |
| CHEMBL5594512 | — | — | 1 | 6.61 |
| CHEMBL5594479 | — | — | 1 | 6.54 |
| CHEMBL5595408 | — | — | 1 | 6.50 |
| CHEMBL5590688 | — | — | 1 | 6.24 |
| CHEMBL5590970 | — | — | 1 | 6.16 |
| CHEMBL5591779 | — | — | 1 | 6.15 |
| CHEMBL5596025 | — | — | 1 | 6.02 |
| CHEMBL5592215 | — | — | 1 | 5.95 |
| CHEMBL5593093 | — | — | 1 | 5.95 |
| CHEMBL5592738 | — | — | 1 | 5.73 |
| CHEMBL5584169 | — | — | 1 | 5.47 |
| CHEMBL5592329 | — | — | 1 | 5.46 |
| CHEMBL5593669 | — | — | 1 | 5.41 |
| CHEMBL5594621 | — | — | 1 | 5.41 |
| CHEMBL5584021 | — | — | 1 | 5.38 |
| CHEMBL5594774 | — | — | 1 | 5.34 |
| CHEMBL5594311 | — | — | 1 | 5.22 |
| CHEMBL3603847 | — | — | 1 | - |
| CHEMBL5592926 | — | — | 1 | - |
| CHEMBL5594272 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3656841 | — | IC50 | = | 3.57 | nM | 8.45 |
| CHEMBL4754493 | BTX-A51 | IC50 | = | 18.62 | nM | 7.73 |
| CHEMBL5590934 | — | IC50 | = | 39.12 | nM | 7.41 |
| CHEMBL5593193 | — | IC50 | = | 93.97 | nM | 7.03 |
| CHEMBL5595728 | — | IC50 | = | 137.75 | nM | 6.86 |
| CHEMBL5593612 | — | IC50 | = | 139.8 | nM | 6.85 |
| CHEMBL5592046 | — | IC50 | = | 168.05 | nM | 6.78 |
| CHEMBL5594512 | — | IC50 | = | 246.8 | nM | 6.61 |
| CHEMBL5594479 | — | IC50 | = | 291.65 | nM | 6.54 |
| CHEMBL5595408 | — | IC50 | = | 313.2 | nM | 6.50 |
| CHEMBL5590688 | — | IC50 | = | 572.7 | nM | 6.24 |
| CHEMBL5590970 | — | IC50 | = | 685.6 | nM | 6.16 |
| CHEMBL5591779 | — | IC50 | = | 704.3 | nM | 6.15 |
| CHEMBL5596025 | — | IC50 | = | 948.05 | nM | 6.02 |
| CHEMBL5592215 | — | IC50 | = | 1130.2 | nM | 5.95 |
| CHEMBL5593093 | — | IC50 | = | 1121.85 | nM | 5.95 |
| CHEMBL5592738 | — | IC50 | = | 1847.0 | nM | 5.73 |
| CHEMBL5584169 | — | IC50 | = | 3419.5 | nM | 5.47 |
| CHEMBL5592329 | — | IC50 | = | 3454.5 | nM | 5.46 |
| CHEMBL5593669 | — | IC50 | = | 3860.5 | nM | 5.41 |
| CHEMBL5594621 | — | IC50 | = | 3922.0 | nM | 5.41 |
| CHEMBL5584021 | — | IC50 | = | 4200.5 | nM | 5.38 |
| CHEMBL5594774 | — | IC50 | = | 4610.5 | nM | 5.34 |
| CHEMBL5594311 | — | IC50 | = | 5993.5 | nM | 5.22 |
| CHEMBL3603847 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5592926 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5594272 | — | IC50 | > | 10000.0 | nM | - |