Assay Detail
Binding
CHEMBL5048666
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Inhibition of full length N-terminal GST fused human CDK7 (1 to 346 residues)/CyclinH (1 to 323 residues)/ MAT1 (1 to 309 residues) expressed in baculovirus expression system using FL peptide as substrate preincubated for 30 mins followed by substrate addition and further incubated for 90 mins by EZ reader method
17
Total Activities
17
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 and Optimization of Highly Selective Inhibitors of CDK5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.68 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080866 | — | — | 1 | 7.14 |
| CHEMBL5078192 | — | — | 1 | 7.11 |
| CHEMBL5088480 | — | — | 1 | 7.06 |
| CHEMBL5077028 | — | — | 1 | 7.03 |
| CHEMBL5091792 | — | — | 1 | 7.02 |
| CHEMBL5080361 | — | — | 1 | 6.98 |
| CHEMBL5090019 | — | — | 1 | 6.83 |
| CHEMBL5070707 | — | — | 1 | 6.79 |
| CHEMBL5080566 | — | — | 1 | 6.77 |
| CHEMBL5088595 | — | — | 1 | 6.71 |
| CHEMBL5087911 | — | — | 1 | 6.53 |
| CHEMBL5079342 | — | — | 1 | 6.48 |
| CHEMBL5083778 | — | — | 1 | 6.44 |
| CHEMBL5080813 | — | — | 1 | 6.20 |
| CHEMBL5084200 | — | — | 1 | 6.14 |
| CHEMBL5084882 | — | — | 1 | 6.14 |
| CHEMBL5080123 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080866 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL5078192 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5088480 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5077028 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5091792 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL5080361 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5090019 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5070707 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5080566 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL5088595 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL5087911 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL5079342 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL5083778 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL5080813 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL5084200 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL5084882 | — | IC50 | = | 729.0 | nM | 6.14 |
| CHEMBL5080123 | — | IC50 | = | 784.0 | nM | 6.11 |