Assay Detail
Binding
CHEMBL3777412
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP
25
Total Activities
25
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
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.01 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775792 | — | — | 1 | 9.00 |
| CHEMBL3774632 | — | — | 1 | 8.30 |
| CHEMBL3775509 | — | — | 1 | 8.30 |
| CHEMBL3775470 | — | — | 1 | 8.10 |
| CHEMBL3774932 | — | — | 1 | 8.05 |
| CHEMBL3775608 | — | — | 1 | 7.77 |
| CHEMBL3775677 | — | — | 1 | 7.68 |
| CHEMBL3774979 | — | — | 1 | 7.43 |
| CHEMBL3775223 | — | — | 1 | 7.36 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 7.35 |
| CHEMBL3775502 | — | — | 1 | 7.31 |
| CHEMBL3775681 | — | — | 1 | 6.94 |
| CHEMBL3774949 | — | — | 1 | 6.92 |
| CHEMBL3775606 | — | — | 1 | 6.78 |
| CHEMBL3774503 | — | — | 1 | 6.75 |
| CHEMBL3774434 | — | — | 1 | 6.74 |
| CHEMBL518800 | — | — | 1 | 6.65 |
| CHEMBL3775479 | — | — | 1 | 6.64 |
| CHEMBL3775467 | — | — | 1 | 6.38 |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | 5.97 |
| CHEMBL3775657 | — | — | 1 | 5.67 |
| CHEMBL3775861 | — | — | 1 | 5.44 |
| CHEMBL1801932 | — | — | 1 | 5.43 |
| CHEMBL3774636 | — | — | 1 | 5.36 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775792 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3774632 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3775509 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3775470 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3774932 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3775608 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3775677 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3774979 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3775223 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2103840 | DINACICLIB | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3775502 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3775681 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3774949 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL3775606 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3774503 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL3774434 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL518800 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL3775479 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL3775467 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL14762 | SELICICLIB | IC50 | = | 1069.0 | nM | 5.97 |
| CHEMBL3775657 | — | IC50 | = | 2136.0 | nM | 5.67 |
| CHEMBL3775861 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1801932 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3774636 | — | IC50 | = | 4415.0 | nM | 5.36 |
| CHEMBL189963 | PALBOCICLIB | IC50 | > | 10000.0 | nM | - |