Assay Detail
Binding
CHEMBL986351
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthalenyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-6-yl]methanesulfonamide from human ERG in HEK293 cells
35
Total Activities
35
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
Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.47 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL476322 | — | — | 1 | 6.46 |
| CHEMBL518431 | — | — | 1 | 6.15 |
| CHEMBL479241 | — | — | 1 | 5.96 |
| CHEMBL478616 | — | — | 1 | 5.80 |
| CHEMBL479252 | — | — | 1 | 5.60 |
| CHEMBL477364 | — | — | 1 | 5.58 |
| CHEMBL515004 | — | — | 1 | 5.55 |
| CHEMBL479036 | — | — | 1 | 5.41 |
| CHEMBL476723 | — | — | 1 | 5.30 |
| CHEMBL478395 | — | — | 1 | 5.28 |
| CHEMBL476106 | — | — | 1 | 5.22 |
| CHEMBL477360 | — | — | 1 | 5.22 |
| CHEMBL515477 | — | — | 1 | 5.19 |
| CHEMBL476579 | — | — | 1 | 5.18 |
| CHEMBL479242 | — | — | 1 | 5.18 |
| CHEMBL478615 | — | — | 1 | 5.17 |
| CHEMBL477363 | — | — | 1 | 5.09 |
| CHEMBL487063 | — | — | 1 | 5.07 |
| CHEMBL477991 | — | — | 1 | - |
| CHEMBL477990 | — | — | 1 | - |
| CHEMBL476323 | MK-0249 | 2.0 | 1 | - |
| CHEMBL478406 | — | — | 1 | - |
| CHEMBL516725 | — | — | 1 | - |
| CHEMBL477201 | — | — | 1 | - |
| CHEMBL477152 | — | — | 1 | - |
| CHEMBL477356 | — | — | 1 | - |
| CHEMBL515150 | — | — | 1 | - |
| CHEMBL477361 | — | — | 1 | - |
| CHEMBL476373 | — | — | 1 | - |
| CHEMBL478621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL476322 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL518431 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL479241 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL478616 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL479252 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL477364 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL515004 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL479036 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL476723 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL478395 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL476106 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL477360 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL515477 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL476579 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL479242 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL478615 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL477363 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL487063 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL515150 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL446516 | — | IC50 | - | — | - | |
| CHEMBL477556 | — | IC50 | - | — | - | |
| CHEMBL516126 | — | IC50 | - | — | - | |
| CHEMBL478628 | — | IC50 | - | — | - | |
| CHEMBL443958 | — | IC50 | - | — | - | |
| CHEMBL478621 | — | IC50 | - | — | - | |
| CHEMBL476373 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL477361 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL477991 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL477356 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL477152 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL477201 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL516725 | — | IC50 | - | — | - | |
| CHEMBL478406 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL476323 | MK-0249 | IC50 | > | 10000.0 | nM | - |
| CHEMBL477990 | — | IC50 | > | 10000.0 | nM | - |