Assay Detail
Binding
CHEMBL4610754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG
42
Total Activities
42
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
Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 5.33 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638334 | — | — | 1 | 5.82 |
| CHEMBL376488 | BEDAQUILINE | 4.0 | 1 | 5.80 |
| CHEMBL4646329 | — | — | 1 | 5.75 |
| CHEMBL4637257 | — | — | 1 | 5.55 |
| CHEMBL4647327 | — | — | 1 | 5.48 |
| CHEMBL4645910 | — | — | 1 | 5.47 |
| CHEMBL4645781 | — | — | 1 | 5.32 |
| CHEMBL4637995 | — | — | 1 | 5.29 |
| CHEMBL4645820 | — | — | 1 | 5.28 |
| CHEMBL4642317 | — | — | 1 | 5.23 |
| CHEMBL4634074 | — | — | 1 | 5.16 |
| CHEMBL4645301 | — | — | 1 | 5.11 |
| CHEMBL4647399 | — | — | 1 | 5.04 |
| CHEMBL4529465 | TBAJ-587 | 1.0 | 1 | 4.89 |
| CHEMBL4640836 | — | — | 1 | 4.77 |
| CHEMBL4639550 | — | — | 1 | - |
| CHEMBL4648576 | — | — | 1 | - |
| CHEMBL4639462 | — | — | 1 | - |
| CHEMBL4633704 | — | — | 1 | - |
| CHEMBL4634386 | — | — | 1 | - |
| CHEMBL4641813 | — | — | 1 | - |
| CHEMBL4641177 | — | — | 1 | - |
| CHEMBL4641852 | — | — | 1 | - |
| CHEMBL4638967 | — | — | 1 | - |
| CHEMBL4647766 | — | — | 1 | - |
| CHEMBL4647741 | — | — | 1 | - |
| CHEMBL4553146 | TBAJ-876 | 2.0 | 1 | - |
| CHEMBL4648337 | — | — | 1 | - |
| CHEMBL4642509 | — | — | 1 | - |
| CHEMBL4634170 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638334 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL376488 | BEDAQUILINE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4646329 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4637257 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4647327 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4645910 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4645781 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4637995 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4645820 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4642317 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4634074 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4645301 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4647399 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4529465 | TBAJ-587 | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4640836 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4639824 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4633025 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4633038 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643476 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4641396 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643771 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641664 | — | IC50 | - | — | - | |
| CHEMBL4634438 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649701 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4645626 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639550 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4648576 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639462 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4633704 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634386 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4641813 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4641177 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641852 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638967 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647766 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647741 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4553146 | TBAJ-876 | IC50 | > | 30000.0 | nM | - |
| CHEMBL4648337 | — | IC50 | - | — | - | |
| CHEMBL4642509 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4634170 | — | IC50 | > | 30000.0 | nM | - |