Assay Detail
Binding
CHEMBL4200746
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]dofetilide from human ERG by high throughput assay
16
Total Activities
16
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 |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.78 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3908521 | — | — | 1 | 8.05 |
| CHEMBL3910823 | — | — | 1 | 6.51 |
| CHEMBL3915183 | — | — | 1 | 5.96 |
| CHEMBL3892952 | — | — | 1 | 5.82 |
| CHEMBL4110570 | — | — | 1 | 5.44 |
| CHEMBL4217428 | — | — | 1 | 5.43 |
| CHEMBL3954214 | — | — | 1 | 5.02 |
| CHEMBL4106732 | — | — | 1 | 4.98 |
| CHEMBL4115154 | — | — | 1 | 4.77 |
| CHEMBL3956542 | — | — | 1 | - |
| CHEMBL3913939 | — | — | 1 | - |
| CHEMBL3898258 | — | — | 1 | - |
| CHEMBL4217559 | — | — | 1 | - |
| CHEMBL4114922 | — | — | 1 | - |
| CHEMBL4213152 | — | — | 1 | - |
| CHEMBL4208229 | ASCIMINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3908521 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3910823 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3915183 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3892952 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4110570 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4217428 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3954214 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4106732 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL4115154 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3956542 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3913939 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3898258 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4217559 | — | IC50 | >= | 23000.0 | nM | - |
| CHEMBL4114922 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4213152 | — | IC50 | >= | 18500.0 | nM | - |
| CHEMBL4208229 | ASCIMINIB | IC50 | > | 30000.0 | nM | - |