Assay Detail
ADMET
CHEMBL4387135
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Inhibition of human recombinant full length GST-tagged CDK1/Cyclin A2 expressed in sf9 insect cells assessed as inhibition constant using Ulight-4E-BP1 as substrate preincubated for 30 mins followed by substrate addition and incubated for 90 mins by TR-FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.46 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1272326 | — | — | 1 | 7.62 |
| CHEMBL4564687 | — | — | 1 | 7.28 |
| CHEMBL4589135 | — | — | 1 | 7.20 |
| CHEMBL4546255 | — | — | 1 | 7.16 |
| CHEMBL4560219 | — | — | 1 | 7.11 |
| CHEMBL4440980 | — | — | 1 | 7.11 |
| CHEMBL4545456 | — | — | 1 | 6.96 |
| CHEMBL4529532 | — | — | 1 | 6.96 |
| CHEMBL4539133 | — | — | 1 | 6.68 |
| CHEMBL4438971 | — | — | 1 | 6.57 |
| CHEMBL4466797 | — | — | 1 | 6.55 |
| CHEMBL4536835 | — | — | 1 | 6.28 |
| CHEMBL4520067 | — | — | 1 | 6.20 |
| CHEMBL4561999 | — | — | 1 | 6.11 |
| CHEMBL4578267 | — | — | 1 | 6.07 |
| CHEMBL4435669 | — | — | 1 | 6.01 |
| CHEMBL4588989 | — | — | 1 | 5.89 |
| CHEMBL4569666 | — | — | 1 | 5.70 |
| CHEMBL4464950 | — | — | 1 | 5.28 |
| CHEMBL4447396 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1272326 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4564687 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4589135 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4546255 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4560219 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4440980 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4545456 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4529532 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL4539133 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4438971 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL4466797 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL4536835 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL4520067 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL4561999 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL4578267 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL4435669 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL4588989 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4569666 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4464950 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL4447396 | — | Ki | = | 29000.0 | nM | 4.54 |