Assay Detail
Binding
CHEMBL4180589
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Inhibition of CDK4 (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 | 8.13 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4208504 | — | — | 1 | 8.82 |
| CHEMBL4218267 | — | — | 1 | 8.80 |
| CHEMBL4202432 | — | — | 1 | 8.80 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.72 |
| CHEMBL4204030 | — | — | 1 | 8.68 |
| CHEMBL4216534 | — | — | 1 | 8.66 |
| CHEMBL4207218 | — | — | 1 | 8.62 |
| CHEMBL4208198 | — | — | 1 | 8.54 |
| CHEMBL4213557 | — | — | 1 | 8.54 |
| CHEMBL4214898 | — | — | 1 | 8.51 |
| CHEMBL4214634 | — | — | 1 | 8.43 |
| CHEMBL4205366 | — | — | 1 | 8.28 |
| CHEMBL4214123 | — | — | 1 | 8.25 |
| CHEMBL4208875 | — | — | 1 | 8.06 |
| CHEMBL4211162 | — | — | 1 | 7.92 |
| CHEMBL4218705 | — | — | 1 | 7.86 |
| CHEMBL4203994 | — | — | 1 | 7.74 |
| CHEMBL4213770 | — | — | 1 | 7.45 |
| CHEMBL4206797 | — | — | 1 | 6.55 |
| CHEMBL4206280 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4208504 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4218267 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4202432 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4204030 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4216534 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4207218 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4208198 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4213557 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4214898 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4214634 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4205366 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4214123 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4208875 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4211162 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL4218705 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4203994 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL4213770 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL4206797 | — | IC50 | = | 283.4 | nM | 6.55 |
| CHEMBL4206280 | — | IC50 | = | 5156.0 | nM | 5.29 |