Assay Detail
Binding
CHEMBL4671572
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Inhibition of human ERG
20
Total Activities
20
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
Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D/D receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.96 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740880 | — | — | 1 | 6.22 |
| CHEMBL4756987 | — | — | 1 | 6.22 |
| CHEMBL4742056 | — | — | 1 | 6.22 |
| CHEMBL4745124 | — | — | 1 | 6.10 |
| CHEMBL4758966 | — | — | 1 | 6.05 |
| CHEMBL4795230 | — | — | 1 | 6.05 |
| CHEMBL4760903 | — | — | 1 | 5.96 |
| CHEMBL4756254 | — | — | 1 | 5.96 |
| CHEMBL4758723 | — | — | 1 | 5.92 |
| CHEMBL4757297 | — | — | 1 | 5.82 |
| CHEMBL4776090 | — | — | 1 | 5.80 |
| CHEMBL4745489 | — | — | 1 | 5.72 |
| CHEMBL42 | CLOZAPINE | 4.0 | 1 | 5.50 |
| CHEMBL715 | OLANZAPINE | 4.0 | 1 | - |
| CHEMBL4779001 | — | — | 1 | - |
| CHEMBL4793813 | — | — | 1 | - |
| CHEMBL4797375 | — | — | 1 | - |
| CHEMBL4784005 | — | — | 1 | - |
| CHEMBL4779083 | — | — | 1 | - |
| CHEMBL4745242 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740880 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4756987 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4742056 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4745124 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4758966 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4795230 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4760903 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4756254 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4758723 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4757297 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4776090 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4745489 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL715 | OLANZAPINE | IC50 | - | — | - | |
| CHEMBL4779001 | — | IC50 | - | — | - | |
| CHEMBL4793813 | — | IC50 | - | — | - | |
| CHEMBL4797375 | — | IC50 | - | — | - | |
| CHEMBL4784005 | — | IC50 | - | — | - | |
| CHEMBL4779083 | — | IC50 | - | — | - | |
| CHEMBL4745242 | — | IC50 | - | — | - |