Assay Detail
Binding
CHEMBL4180590
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Inhibition of CDK1 (unknown origin) using U-light as substrate preincubated for 1 hr followed by EDTA addition measured after 1 hr by LANCE Ultra kinase assay
20
Total Activities
20
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
Discovery of a class of diheteroaromatic amines as orally bioavailable CDK1/4/6 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.48 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204030 | — | — | 1 | 7.45 |
| CHEMBL4218267 | — | — | 1 | 7.36 |
| CHEMBL4202432 | — | — | 1 | 7.01 |
| CHEMBL4216534 | — | — | 1 | 7.00 |
| CHEMBL4213557 | — | — | 1 | 6.99 |
| CHEMBL4208504 | — | — | 1 | 6.87 |
| CHEMBL4207218 | — | — | 1 | 6.87 |
| CHEMBL4214634 | — | — | 1 | 6.86 |
| CHEMBL4214123 | — | — | 1 | 6.82 |
| CHEMBL4208875 | — | — | 1 | 6.64 |
| CHEMBL4208198 | — | — | 1 | 6.52 |
| CHEMBL4214898 | — | — | 1 | 6.38 |
| CHEMBL4205366 | — | — | 1 | 6.10 |
| CHEMBL4203994 | — | — | 1 | 5.85 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 5.82 |
| CHEMBL4211162 | — | — | 1 | 5.78 |
| CHEMBL4218705 | — | — | 1 | 5.61 |
| CHEMBL4213770 | — | — | 1 | 4.69 |
| CHEMBL4206797 | — | — | 1 | - |
| CHEMBL4206280 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204030 | — | IC50 | = | 35.8 | nM | 7.45 |
| CHEMBL4218267 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4202432 | — | IC50 | = | 97.2 | nM | 7.01 |
| CHEMBL4216534 | — | IC50 | = | 100.5 | nM | 7.00 |
| CHEMBL4213557 | — | IC50 | = | 103.1 | nM | 6.99 |
| CHEMBL4208504 | — | IC50 | = | 135.5 | nM | 6.87 |
| CHEMBL4207218 | — | IC50 | = | 133.8 | nM | 6.87 |
| CHEMBL4214634 | — | IC50 | = | 139.7 | nM | 6.86 |
| CHEMBL4214123 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4208875 | — | IC50 | = | 230.7 | nM | 6.64 |
| CHEMBL4208198 | — | IC50 | = | 300.9 | nM | 6.52 |
| CHEMBL4214898 | — | IC50 | = | 411.9 | nM | 6.38 |
| CHEMBL4205366 | — | IC50 | = | 800.9 | nM | 6.10 |
| CHEMBL4203994 | — | IC50 | = | 1413.0 | nM | 5.85 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1523.0 | nM | 5.82 |
| CHEMBL4211162 | — | IC50 | = | 1671.1 | nM | 5.78 |
| CHEMBL4218705 | — | IC50 | = | 2429.5 | nM | 5.61 |
| CHEMBL4213770 | — | IC50 | = | 20225.0 | nM | 4.69 |
| CHEMBL4206797 | — | IC50 | - | — | - | |
| CHEMBL4206280 | — | IC50 | - | — | - |