Assay Detail
Binding
CHEMBL2168489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human ERG expressed in CHOK1 cells by IonWorks HT assay
62
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 5.02 | 5.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164359 | — | — | 1 | 5.48 |
| CHEMBL2164037 | — | — | 1 | 5.44 |
| CHEMBL2164361 | — | — | 1 | 5.37 |
| CHEMBL2164389 | — | — | 3 | 5.34 |
| CHEMBL2164358 | — | — | 1 | 5.31 |
| CHEMBL2164046 | — | — | 1 | 5.29 |
| CHEMBL2164047 | — | — | 1 | 5.28 |
| CHEMBL2164382 | — | — | 1 | 5.26 |
| CHEMBL2164366 | — | — | 1 | 5.26 |
| CHEMBL2164369 | — | — | 1 | 5.25 |
| CHEMBL2164368 | — | — | 1 | 5.25 |
| CHEMBL2164356 | — | — | 1 | 5.18 |
| CHEMBL2164393 | — | — | 1 | 5.14 |
| CHEMBL2164039 | — | — | 1 | 5.09 |
| CHEMBL2164360 | — | — | 1 | 5.07 |
| CHEMBL2164387 | — | — | 1 | 5.07 |
| CHEMBL2164392 | — | — | 1 | 5.05 |
| CHEMBL2164365 | — | — | 1 | 5.04 |
| CHEMBL2164384 | — | — | 1 | 5.03 |
| CHEMBL2164363 | — | — | 1 | 5.01 |
| CHEMBL2164375 | — | — | 1 | 4.96 |
| CHEMBL2164367 | — | — | 3 | 4.96 |
| CHEMBL2164374 | — | — | 1 | 4.85 |
| CHEMBL2164373 | — | — | 3 | 4.85 |
| CHEMBL2164391 | — | — | 1 | 4.85 |
| CHEMBL2164364 | — | — | 1 | 4.80 |
| CHEMBL2164395 | — | — | 1 | 4.80 |
| CHEMBL2164372 | — | — | 1 | 4.77 |
| CHEMBL2164396 | — | — | 1 | 4.70 |
| CHEMBL2164390 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164359 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2164037 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2164361 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2164389 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL2164358 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2164046 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2164047 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2164382 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2164366 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL2164369 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL2164368 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL2164356 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2164393 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL2164389 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL2164039 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL2164387 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2164360 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL2164392 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL2164365 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL2164384 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL2164363 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL2164367 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2164375 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2164374 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2164391 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2164373 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL2164395 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2164364 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2164372 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2164396 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2164390 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL2164397 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL2164376 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2164042 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2164381 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL2164380 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2164038 | — | IC50 | - | — | - | |
| CHEMBL2164040 | — | IC50 | - | — | - | |
| CHEMBL2164041 | — | IC50 | - | — | - | |
| CHEMBL2164043 | — | IC50 | - | — | - | |
| CHEMBL2164044 | — | IC50 | > | 33000.0 | nM | - |
| CHEMBL2164357 | — | IC50 | - | — | - | |
| CHEMBL2164383 | — | IC50 | - | — | - | |
| CHEMBL2164385 | — | IC50 | - | — | - | |
| CHEMBL2164386 | — | IC50 | - | — | - | |
| CHEMBL2164388 | — | IC50 | - | — | - | |
| CHEMBL2164389 | — | IC50 | - | — | - | |
| CHEMBL2164394 | — | IC50 | - | — | - | |
| CHEMBL2164370 | — | IC50 | - | — | - | |
| CHEMBL2164378 | — | IC50 | - | — | - |