Assay Detail
ADMET
CHEMBL4325177
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Inhibition of human CDK4 using biotinylated-aminohexyl-Ala-Ala-Ala-Lys-Arg-Arg-Glu-Ile-Leu-Ser-Arg-Arg-Pro-Ser(PO3)-Tyr-Arg-amide as substrate after 40 mins in presence of [gamma-32P]ATP by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-<i>b</i>]pyridazines for the Treatment of Human African Trypanosomiasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.62 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359999 | GW801372X | — | 1 | 7.70 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | — | 1 | 7.20 |
| CHEMBL359554 | — | — | 1 | 6.80 |
| CHEMBL361894 | GW806290X | — | 1 | 6.50 |
| CHEMBL186101 | — | — | 1 | 5.80 |
| CHEMBL364587 | — | — | 1 | 5.70 |
| CHEMBL365248 | GW810372X | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359999 | GW801372X | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL359554 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL361894 | GW806290X | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL186101 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL364587 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL365248 | GW810372X | IC50 | > | 19952.62 | nM | - |