Assay Detail
Binding
CHEMBL4742550
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Inhibition of CDK12 (unknown origin) using ULight - 4E - BP1( Thr37 / Thr46 ) as substrate preincubated for 60 mins bu LANCE-TR-FRET assay
46
Total Activities
37
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 | 46 | 6.99 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4777061 | — | — | 1 | 8.40 |
| CHEMBL4799386 | — | — | 1 | 8.22 |
| CHEMBL4792293 | — | — | 2 | 8.05 |
| CHEMBL4797074 | — | — | 1 | 8.00 |
| CHEMBL4784107 | — | — | 1 | 7.92 |
| CHEMBL4783704 | — | — | 1 | 7.85 |
| CHEMBL4791883 | — | — | 1 | 7.64 |
| CHEMBL4781207 | — | — | 3 | 7.54 |
| CHEMBL4778676 | — | — | 3 | 7.50 |
| CHEMBL4786926 | — | — | 1 | 7.43 |
| CHEMBL4791767 | — | — | 1 | 7.40 |
| CHEMBL4778361 | — | — | 3 | 7.40 |
| CHEMBL4778572 | — | — | 1 | 7.39 |
| CHEMBL4794547 | — | — | 1 | 7.31 |
| CHEMBL4776295 | — | — | 1 | 7.26 |
| CHEMBL4790705 | — | — | 1 | 7.24 |
| CHEMBL4777358 | — | — | 1 | 7.22 |
| CHEMBL4778214 | — | — | 1 | 7.08 |
| CHEMBL4784925 | — | — | 1 | 7.03 |
| CHEMBL4781396 | — | — | 1 | 7.00 |
| CHEMBL4799777 | — | — | 1 | 6.85 |
| CHEMBL4800122 | — | — | 1 | 6.82 |
| CHEMBL4792842 | — | — | 1 | 6.80 |
| CHEMBL4793480 | — | — | 1 | 6.75 |
| CHEMBL4798660 | — | — | 1 | 6.75 |
| CHEMBL4788447 | — | — | 1 | 6.72 |
| CHEMBL4782687 | — | — | 1 | 6.69 |
| CHEMBL4794718 | — | — | 1 | 6.64 |
| CHEMBL4787409 | — | — | 1 | 6.63 |
| CHEMBL4786663 | — | — | 1 | 6.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4777061 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4799386 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4792293 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4797074 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4784107 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4783704 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4791883 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4781207 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4781207 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4778676 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4778676 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4786926 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4791767 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4778361 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4778572 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4794547 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4776295 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4790705 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4777358 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4778361 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4778214 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4784925 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4781396 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4799777 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4800122 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4792842 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4793480 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4798660 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4788447 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4782687 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4794718 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4787409 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL4786663 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL4779633 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4781668 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4780788 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4800324 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4792293 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL4781668 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4788085 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL4778676 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL4781207 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL4779066 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4785443 | — | IC50 | = | 895.0 | nM | 6.05 |
| CHEMBL4779066 | — | IC50 | = | 1019.0 | nM | 5.99 |
| CHEMBL4778361 | — | IC50 | = | 1309.0 | nM | 5.88 |