Assay Detail
Binding
CHEMBL3859635
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Inhibition of human ERG
8
Total Activities
8
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 Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.93 | 5.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3970692 | — | — | 1 | 5.44 |
| CHEMBL3927522 | — | — | 1 | 5.27 |
| CHEMBL3927609 | — | — | 1 | 4.77 |
| CHEMBL3972563 | — | — | 1 | 4.64 |
| CHEMBL3980602 | — | — | 1 | 4.51 |
| CHEMBL3900409 | BRENSOCATIB | 3.0 | 1 | - |
| CHEMBL3960432 | — | — | 1 | - |
| CHEMBL3891374 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3970692 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3927522 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3927609 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3972563 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3980602 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL3900409 | BRENSOCATIB | IC50 | > | 33000.0 | nM | - |
| CHEMBL3960432 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL3891374 | — | IC50 | > | 33000.0 | nM | - |