Assay Detail
Binding
CHEMBL3090534
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
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 and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.37 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086045 | — | — | 1 | 8.52 |
| CHEMBL3086035 | — | — | 1 | 7.41 |
| CHEMBL3086036 | — | — | 1 | 7.00 |
| CHEMBL3086047 | — | — | 1 | 6.77 |
| CHEMBL3086041 | — | — | 1 | 6.75 |
| CHEMBL3086029 | — | — | 1 | 6.54 |
| CHEMBL3086048 | — | — | 1 | 6.28 |
| CHEMBL3086040 | — | — | 1 | 6.23 |
| CHEMBL3086039 | — | — | 1 | 6.16 |
| CHEMBL3086028 | — | — | 1 | 6.11 |
| CHEMBL3086042 | — | — | 1 | 6.00 |
| CHEMBL3086043 | — | — | 1 | 5.92 |
| CHEMBL3086038 | — | — | 1 | 5.82 |
| CHEMBL3086037 | — | — | 1 | 5.72 |
| CHEMBL3086032 | — | — | 1 | 5.66 |
| CHEMBL3085780 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086045 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3086035 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3086036 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3086047 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3086041 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3086029 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3086048 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3086040 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3086039 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3086028 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3086042 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3086043 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3086038 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3086037 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3086032 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3085780 | — | IC50 | = | 8400.0 | nM | 5.08 |