Assay Detail
Binding
CHEMBL827377
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Binding affinity for human cyclin-dependent kinase 2
91
Total Activities
91
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 | 91 | 7.29 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL359794 | — | — | 1 | 9.00 |
| CHEMBL184510 | — | — | 1 | 9.00 |
| CHEMBL186890 | — | — | 1 | 9.00 |
| CHEMBL364370 | — | — | 1 | 8.70 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | — | 1 | 8.70 |
| CHEMBL186101 | — | — | 1 | 8.52 |
| CHEMBL359554 | — | — | 1 | 8.30 |
| CHEMBL186708 | — | — | 1 | 8.22 |
| CHEMBL361894 | GW806290X | — | 1 | 8.22 |
| CHEMBL434337 | — | — | 1 | 8.22 |
| CHEMBL187750 | — | — | 1 | 8.10 |
| CHEMBL188665 | — | — | 1 | 8.00 |
| CHEMBL189455 | — | — | 1 | 8.00 |
| CHEMBL359999 | GW801372X | — | 1 | 8.00 |
| CHEMBL365229 | — | — | 1 | 8.00 |
| CHEMBL359963 | GW805758X | — | 1 | 8.00 |
| CHEMBL360206 | — | — | 1 | 8.00 |
| CHEMBL188938 | — | — | 1 | 7.70 |
| CHEMBL186680 | — | — | 1 | 7.70 |
| CHEMBL186288 | — | — | 1 | 7.70 |
| CHEMBL187006 | — | — | 1 | 7.30 |
| CHEMBL186054 | PYRAZOLOPYRIDAZINE 2 | — | 1 | 7.30 |
| CHEMBL188312 | — | — | 1 | 7.22 |
| CHEMBL188785 | — | — | 1 | 7.00 |
| CHEMBL185871 | — | — | 1 | 6.82 |
| CHEMBL364587 | — | — | 1 | 6.82 |
| CHEMBL189235 | — | — | 1 | 6.80 |
| CHEMBL188303 | — | — | 1 | 6.72 |
| CHEMBL365248 | GW810372X | — | 1 | 6.72 |
| CHEMBL188417 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL359794 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL186890 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL184510 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL364370 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL187081 | PYRAZOLOPYRIDAZINE 1 | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL186101 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL359554 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL186708 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL361894 | GW806290X | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL434337 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL187750 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL365229 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL189455 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL188665 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL359999 | GW801372X | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL359963 | GW805758X | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL360206 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL188938 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL186680 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL186288 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL187006 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL186054 | PYRAZOLOPYRIDAZINE 2 | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL188312 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL188785 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL364587 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL185871 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL189235 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL188303 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL365248 | GW810372X | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL188417 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL361697 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL189352 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL187139 | — | Ki | = | 790.0 | nM | 6.10 |
| CHEMBL187287 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL183993 | GW811761X | Ki | = | 1990.0 | nM | 5.70 |
| CHEMBL189415 | GW819077X | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL362296 | — | Ki | = | 3980.0 | nM | 5.40 |
| CHEMBL360408 | — | Ki | = | 3980.0 | nM | 5.40 |
| CHEMBL189617 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL360866 | — | Ki | = | 19900.0 | nM | 4.70 |
| CHEMBL186116 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL189343 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL434729 | GW829906X | Ki | > | 19950.0 | nM | - |
| CHEMBL186166 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL189288 | — | Ki | > | 19950.0 | nM | - |
| CHEMBL365297 | GW827099X | Ki | > | 19950.0 | nM | - |
| CHEMBL186213 | GW827105X | Ki | > | 19950.0 | nM | - |
| CHEMBL427159 | GW827396X | Ki | > | 19950.0 | nM | - |
| CHEMBL188794 | GW829115X | Ki | > | 19950.0 | nM | - |
| CHEMBL188257 | GW827106X | Ki | > | 19950.0 | nM | - |