Assay Detail
Binding
CHEMBL4742552
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Inhibition of CDK7 (unknown origin) using ULight -mylein basic protein as substrate preincubated for 60 mins bu LANCE-TR-FRET assay
27
Total Activities
22
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
Substituted Pyrazole Derivatives As Selective CDK12/13 Inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.82 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784656 | — | — | 1 | 7.92 |
| CHEMBL4781207 | — | — | 1 | 6.82 |
| CHEMBL4783704 | — | — | 1 | 6.36 |
| CHEMBL4799698 | — | — | 1 | 6.30 |
| CHEMBL4787409 | — | — | 1 | 6.21 |
| CHEMBL4790458 | — | — | 1 | 6.13 |
| CHEMBL4792293 | — | — | 2 | 6.06 |
| CHEMBL4778676 | — | — | 1 | 6.00 |
| CHEMBL4778361 | — | — | 3 | 5.89 |
| CHEMBL4782687 | — | — | 1 | 5.77 |
| CHEMBL4776295 | — | — | 1 | 5.76 |
| CHEMBL4781396 | — | — | 1 | 5.68 |
| CHEMBL4794718 | — | — | 1 | 5.66 |
| CHEMBL4777358 | — | — | 1 | 5.64 |
| CHEMBL4781668 | — | — | 2 | 5.63 |
| CHEMBL4800122 | — | — | 1 | 5.55 |
| CHEMBL4778214 | — | — | 1 | 5.48 |
| CHEMBL4780788 | — | — | 1 | 5.46 |
| CHEMBL4779066 | — | — | 2 | 5.44 |
| CHEMBL4779633 | — | — | 1 | 5.18 |
| CHEMBL4797074 | — | — | 1 | 5.11 |
| CHEMBL4790705 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784656 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4781207 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4783704 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4799698 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL4787409 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL4790458 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL4792293 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4778676 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4778361 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4778361 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL4782687 | — | IC50 | = | 1692.0 | nM | 5.77 |
| CHEMBL4776295 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL4781396 | — | IC50 | = | 2090.0 | nM | 5.68 |
| CHEMBL4794718 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL4777358 | — | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL4781668 | — | IC50 | = | 2322.0 | nM | 5.63 |
| CHEMBL4800122 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL4778214 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4780788 | — | IC50 | = | 3510.0 | nM | 5.46 |
| CHEMBL4779066 | — | IC50 | = | 3646.0 | nM | 5.44 |
| CHEMBL4779066 | — | IC50 | = | 5492.0 | nM | 5.26 |
| CHEMBL4792293 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL4779633 | — | IC50 | = | 6585.0 | nM | 5.18 |
| CHEMBL4797074 | — | IC50 | = | 7790.0 | nM | 5.11 |
| CHEMBL4781668 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL4790705 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4778361 | — | IC50 | > | 10000.0 | nM | - |