Assay Detail
Binding
CHEMBL3102091
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK cells after 3 hrs by ion flux electrophysiology
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Structure activity relationships of fused bicyclic and urea derivatives of spirocyclic compounds as potent CCR1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.91 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099950 | — | — | 1 | 6.40 |
| CHEMBL3099949 | — | — | 1 | 6.40 |
| CHEMBL3099952 | — | — | 1 | 6.30 |
| CHEMBL3099953 | — | — | 1 | 6.22 |
| CHEMBL3099951 | — | — | 1 | 6.22 |
| CHEMBL3099944 | — | — | 1 | 6.16 |
| CHEMBL3099943 | — | — | 1 | 6.00 |
| CHEMBL3099958 | — | — | 1 | 5.96 |
| CHEMBL3099959 | — | — | 1 | 5.92 |
| CHEMBL3099945 | — | — | 1 | 5.62 |
| CHEMBL3099947 | — | — | 1 | 5.42 |
| CHEMBL3099942 | — | — | 1 | 5.34 |
| CHEMBL3099961 | — | — | 1 | 4.88 |
| CHEMBL3099948 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099950 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3099949 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3099952 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3099953 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3099951 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3099944 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3099943 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3099958 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3099959 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3099945 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3099947 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3099942 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3099961 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL3099948 | — | IC50 | > | 8900.0 | nM | - |