Assay Detail
Binding
CHEMBL4736826
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Inhibition of tracer 222 binding to GAK (unknown origin) incubated for 1 hr by Lanthascreen TR-FRET assay
27
Total Activities
27
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
Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.33 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740761 | — | — | 1 | 8.66 |
| CHEMBL4778276 | — | — | 1 | 8.49 |
| CHEMBL4762694 | — | — | 1 | 8.42 |
| CHEMBL4764705 | — | — | 1 | 8.11 |
| CHEMBL4794323 | — | — | 1 | 8.06 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.96 |
| CHEMBL4745919 | — | — | 1 | 7.92 |
| CHEMBL4745028 | — | — | 1 | 7.89 |
| CHEMBL4800032 | — | — | 1 | 7.85 |
| CHEMBL4779229 | — | — | 1 | 7.77 |
| CHEMBL4752286 | — | — | 1 | 7.46 |
| CHEMBL4784439 | — | — | 1 | 7.43 |
| CHEMBL4755134 | — | — | 1 | 7.41 |
| CHEMBL3425867 | — | — | 1 | 7.29 |
| CHEMBL4790097 | — | — | 1 | 7.21 |
| CHEMBL4760106 | — | — | 1 | 7.16 |
| CHEMBL4782363 | — | — | 1 | 7.13 |
| CHEMBL4753946 | — | — | 1 | 7.11 |
| CHEMBL4756485 | — | — | 1 | 7.11 |
| CHEMBL4799769 | — | — | 1 | 7.07 |
| CHEMBL4777592 | — | — | 1 | 6.72 |
| CHEMBL4747444 | — | — | 1 | 6.44 |
| CHEMBL4800155 | — | — | 1 | 6.30 |
| CHEMBL4798132 | — | — | 1 | 6.05 |
| CHEMBL4745993 | — | — | 1 | 5.77 |
| CHEMBL4759566 | — | — | 1 | 5.75 |
| CHEMBL4782593 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740761 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4778276 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4762694 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4764705 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4794323 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4745919 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4745028 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4800032 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4779229 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4752286 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4784439 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4755134 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3425867 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4790097 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4760106 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4782363 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4753946 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4756485 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4799769 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4777592 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4747444 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4800155 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4798132 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4745993 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4759566 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4782593 | — | IC50 | > | 1100.0 | nM | - |