Assay Detail
Binding
CHEMBL4610426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tracer 222 binding to recombinant human GST-tagged GAK (1 to 329 residues) expressed in insect cells incubated for 1 hr by Lanthascreen assay
33
Total Activities
33
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
Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.80 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4646895 | — | — | 1 | 7.66 |
| CHEMBL4642467 | — | — | 1 | 7.62 |
| CHEMBL4172550 | — | — | 1 | 7.41 |
| CHEMBL4645917 | — | — | 1 | 7.38 |
| CHEMBL4642620 | — | — | 1 | 7.15 |
| CHEMBL4636314 | — | — | 1 | 7.14 |
| CHEMBL4643096 | — | — | 1 | 7.08 |
| CHEMBL4641825 | — | — | 1 | 7.00 |
| CHEMBL4632903 | — | — | 1 | 7.00 |
| CHEMBL4639991 | — | — | 1 | 6.96 |
| CHEMBL4638602 | — | — | 1 | 6.95 |
| CHEMBL4632372 | — | — | 1 | 6.93 |
| CHEMBL4633404 | — | — | 1 | 6.91 |
| CHEMBL4642058 | — | — | 1 | 6.90 |
| CHEMBL4640730 | — | — | 1 | 6.88 |
| CHEMBL4635935 | — | — | 1 | 6.87 |
| CHEMBL3425876 | — | — | 1 | 6.87 |
| CHEMBL4640641 | — | — | 1 | 6.76 |
| CHEMBL4648802 | — | — | 1 | 6.67 |
| CHEMBL4638387 | — | — | 1 | 6.58 |
| CHEMBL4648554 | — | — | 1 | 6.44 |
| CHEMBL4635431 | — | — | 1 | 6.43 |
| CHEMBL4637058 | — | — | 1 | 6.38 |
| CHEMBL4634338 | — | — | 1 | 6.34 |
| CHEMBL4636735 | — | — | 1 | 6.26 |
| CHEMBL4642436 | — | — | 1 | 6.18 |
| CHEMBL4639109 | — | — | 1 | 5.89 |
| CHEMBL4636582 | — | — | 1 | 5.79 |
| CHEMBL4648514 | — | — | 1 | - |
| CHEMBL4644472 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4646895 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4642467 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4172550 | — | IC50 | = | 39.4 | nM | 7.41 |
| CHEMBL4645917 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4642620 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4636314 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4643096 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4641825 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4632903 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4639991 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4638602 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4632372 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4633404 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4642058 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4640730 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL3425876 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4635935 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4640641 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL4648802 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL4638387 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL4648554 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL4635431 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4637058 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL4634338 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL4636735 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL4642436 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL4639109 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4636582 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4648514 | — | IC50 | > | 370.0 | nM | - |
| CHEMBL4644472 | — | IC50 | > | 370.0 | nM | - |
| CHEMBL4642223 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638607 | — | IC50 | > | 3330.0 | nM | - |
| CHEMBL4648166 | — | IC50 | > | 3330.0 | nM | - |