Assay Detail
Binding
CHEMBL827378
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Binding affinity for human cyclin-dependent kinase 4
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.75 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188665 | — | — | 1 | 8.00 |
| CHEMBL361894 | GW806290X | — | 1 | 8.00 |
| CHEMBL359999 | GW801372X | — | 1 | 8.00 |
| CHEMBL188938 | — | — | 1 | 7.70 |
| CHEMBL187006 | — | — | 1 | 7.52 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | — | 1 | 7.22 |
| CHEMBL359794 | — | — | 1 | 7.22 |
| CHEMBL184510 | — | — | 1 | 7.22 |
| CHEMBL434337 | — | — | 1 | 7.16 |
| CHEMBL186288 | — | — | 1 | 7.00 |
| CHEMBL359554 | — | — | 1 | 6.82 |
| CHEMBL189352 | — | — | 1 | 6.82 |
| CHEMBL186054 | PYRAZOLOPYRIDAZINE 2 | — | 1 | 6.72 |
| CHEMBL360206 | — | — | 1 | 6.72 |
| CHEMBL365229 | — | — | 1 | 6.60 |
| CHEMBL186708 | — | — | 1 | 6.51 |
| CHEMBL185871 | — | — | 1 | 6.51 |
| CHEMBL186680 | — | — | 1 | 6.41 |
| CHEMBL189455 | — | — | 1 | 6.10 |
| CHEMBL186101 | — | — | 1 | 5.80 |
| CHEMBL188785 | — | — | 1 | 5.80 |
| CHEMBL361697 | — | — | 1 | 5.70 |
| CHEMBL364587 | — | — | 1 | 5.70 |
| CHEMBL186890 | — | — | 1 | 5.70 |
| CHEMBL359963 | GW805758X | — | 1 | 5.70 |
| CHEMBL189235 | — | — | 1 | - |
| CHEMBL188312 | — | — | 1 | - |
| CHEMBL365248 | GW810372X | — | 1 | - |
| CHEMBL188417 | — | — | 1 | - |
| CHEMBL187139 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188665 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL361894 | GW806290X | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL359999 | GW801372X | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL188938 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL187006 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL359794 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL184510 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL434337 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL186288 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL359554 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL189352 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL186054 | PYRAZOLOPYRIDAZINE 2 | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL360206 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL365229 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL186708 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL185871 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL186680 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL189455 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL186101 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL188785 | — | Ki | = | 1580.0 | nM | 5.80 |
| CHEMBL361697 | — | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL364587 | — | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL186890 | — | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL359963 | GW805758X | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL189235 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL188312 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL365248 | GW810372X | Ki | > | 19950.0 | nM | - |
| CHEMBL188417 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL187139 | — | Ki | > | 19950.0 | nM | - |