Assay Detail
Binding
CHEMBL2060137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in CHO cells after 30 mins by Rb+ flux assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.21 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 5.96 |
| CHEMBL2059323 | — | — | 1 | 5.72 |
| CHEMBL2059304 | OXIPEROMIDE | 2.0 | 1 | 5.68 |
| CHEMBL2059318 | — | — | 1 | 5.47 |
| CHEMBL2059324 | — | — | 1 | 5.47 |
| CHEMBL2059305 | — | — | 1 | 5.36 |
| CHEMBL2059322 | — | — | 1 | 5.36 |
| CHEMBL2059317 | — | — | 1 | 5.28 |
| CHEMBL2059319 | — | — | 1 | 5.24 |
| CHEMBL2059310 | — | — | 1 | 5.20 |
| CHEMBL2059321 | — | — | 1 | 5.20 |
| CHEMBL2059311 | — | — | 1 | 5.18 |
| CHEMBL2059306 | — | — | 1 | 5.14 |
| CHEMBL2059320 | — | — | 1 | 5.10 |
| CHEMBL2059312 | — | — | 1 | 5.03 |
| CHEMBL2059313 | — | — | 1 | 4.89 |
| CHEMBL1242923 | — | — | 1 | 4.70 |
| CHEMBL2059316 | — | — | 1 | 4.66 |
| CHEMBL2059315 | — | — | 1 | 4.34 |
| CHEMBL2059307 | — | — | 1 | - |
| CHEMBL2059308 | — | — | 1 | - |
| CHEMBL2059309 | — | — | 1 | - |
| CHEMBL2059314 | — | — | 1 | - |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2059323 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2059304 | OXIPEROMIDE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2059318 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2059324 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL2059305 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2059322 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2059317 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2059319 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL2059310 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2059321 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2059311 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2059306 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL2059320 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2059312 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL2059313 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1242923 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2059316 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2059315 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL2059307 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2059308 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2059309 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2059314 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL667 | ACETYLCHOLINE | IC50 | - | — | - |