Assay Detail
Binding
CHEMBL3861882
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO cells assessed as reduction in channel currents at -80 mV holding potential by automated whole-cell patch clamp method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.13 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 5.16 |
| CHEMBL3895337 | — | — | 1 | 5.16 |
| CHEMBL3681314 | — | — | 1 | 5.07 |
| CHEMBL3891894 | — | — | 1 | - |
| CHEMBL3681278 | — | — | 1 | - |
| CHEMBL3681317 | — | — | 1 | - |
| CHEMBL3676329 | — | — | 1 | - |
| CHEMBL3681244 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3895337 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3681314 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3891894 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3681278 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3681317 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3676329 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3681244 | — | IC50 | > | 10000.0 | nM | - |