Assay Detail
Binding
CHEMBL5547017
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis
44
Total Activities
41
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.14 | 8.52 |
| Ki | 12 | 8.21 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5573062 | — | — | 2 | 8.77 |
| CHEMBL5571052 | — | — | 1 | 8.68 |
| CHEMBL5571158 | — | — | 1 | 8.66 |
| CHEMBL5573958 | — | — | 1 | 8.54 |
| CHEMBL5569632 | — | — | 1 | 8.52 |
| CHEMBL4297488 | CT-7001 | 2.0 | 1 | 8.49 |
| CHEMBL5573301 | — | — | 2 | 8.47 |
| CHEMBL5589668 | — | — | 1 | 8.43 |
| CHEMBL5594541 | — | — | 2 | 8.42 |
| CHEMBL5574336 | — | — | 1 | 8.12 |
| CHEMBL5593172 | — | — | 1 | 7.82 |
| CHEMBL5565372 | — | — | 1 | 7.70 |
| CHEMBL5570473 | — | — | 1 | 7.68 |
| CHEMBL5573070 | — | — | 1 | 7.66 |
| CHEMBL5590563 | — | — | 1 | 7.62 |
| CHEMBL5564220 | — | — | 1 | 7.60 |
| CHEMBL5575006 | — | — | 1 | 7.60 |
| CHEMBL5569825 | — | — | 1 | 7.58 |
| CHEMBL5564179 | — | — | 1 | 7.57 |
| CHEMBL5574705 | — | — | 1 | 7.53 |
| CHEMBL5573306 | — | — | 1 | 7.48 |
| CHEMBL5572757 | — | — | 1 | 7.47 |
| CHEMBL5590419 | — | — | 1 | 7.41 |
| CHEMBL5566440 | — | — | 1 | 7.36 |
| CHEMBL5572932 | — | — | 1 | 7.35 |
| CHEMBL5574861 | — | — | 1 | 7.14 |
| CHEMBL5595093 | — | — | 1 | 7.12 |
| CHEMBL5570313 | — | — | 1 | 7.03 |
| CHEMBL5569486 | — | — | 1 | 6.55 |
| CHEMBL5566886 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5573062 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL5571052 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL5571158 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL5573958 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL5569632 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5573062 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4297488 | CT-7001 | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL5573301 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL5589668 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5594541 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL5573301 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5594541 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5574336 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5593172 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5565372 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5570473 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5573070 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5590563 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5564220 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL5575006 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5569825 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5564179 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5574705 | — | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL5573306 | — | Ki | = | 32.9 | nM | 7.48 |
| CHEMBL5572757 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5590419 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5566440 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5572932 | — | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL5574861 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5595093 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5570313 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5569486 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL5566886 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL5562533 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5569232 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5574240 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5568987 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL5572743 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL5571614 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL5575885 | — | IC50 | = | 699.0 | nM | 6.16 |
| CHEMBL5563801 | — | IC50 | = | 807.0 | nM | 6.09 |
| CHEMBL5572224 | — | IC50 | = | 1413.0 | nM | 5.85 |
| CHEMBL5569930 | — | IC50 | = | 4578.0 | nM | 5.34 |
| CHEMBL5574742 | — | IC50 | > | 10000.0 | nM | - |