Assay Detail
Binding
CHEMBL4154412
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced channel currents treated extracellularly after 60 secs by whole cell patch clamp electrophysiology method
26
Total Activities
26
Compounds Tested
2
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
Transient receptor potential cation channel subfamily M member 2 (CHEMBL1250402) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.59 | 6.50 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL173443 | — | — | 1 | 6.50 |
| CHEMBL4176916 | — | — | 1 | 5.43 |
| CHEMBL4159037 | — | — | 1 | 5.40 |
| CHEMBL4174768 | — | — | 1 | 5.34 |
| CHEMBL4167784 | — | — | 1 | 5.29 |
| CHEMBL752 | ADENOSINE PHOSPHATE | 4.0 | 1 | - |
| CHEMBL4161355 | — | — | 1 | - |
| CHEMBL4169283 | — | — | 1 | - |
| CHEMBL4171313 | — | — | 1 | - |
| CHEMBL4166870 | — | — | 1 | - |
| CHEMBL4161542 | — | — | 1 | - |
| CHEMBL4163875 | — | — | 1 | - |
| CHEMBL4164278 | — | — | 1 | - |
| CHEMBL4175597 | — | — | 1 | - |
| CHEMBL4160941 | — | — | 1 | - |
| CHEMBL4174702 | — | — | 1 | - |
| CHEMBL4166935 | — | — | 1 | - |
| CHEMBL4161390 | — | — | 1 | - |
| CHEMBL4164806 | — | — | 1 | - |
| CHEMBL4175434 | — | — | 1 | - |
| CHEMBL4173121 | — | — | 1 | - |
| CHEMBL4165219 | — | — | 1 | - |
| CHEMBL4176311 | — | — | 1 | - |
| CHEMBL4163214 | — | — | 1 | - |
| CHEMBL4167763 | — | — | 1 | - |
| CHEMBL4167493 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL173443 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4176916 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4159037 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4174768 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4167784 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL752 | ADENOSINE PHOSPHATE | Inhibition | - | % | - | |
| CHEMBL4161355 | — | IC50 | - | — | - | |
| CHEMBL4169283 | — | IC50 | - | — | - | |
| CHEMBL4171313 | — | IC50 | - | — | - | |
| CHEMBL4166870 | — | IC50 | - | — | - | |
| CHEMBL4161542 | — | IC50 | - | — | - | |
| CHEMBL4163875 | — | IC50 | - | — | - | |
| CHEMBL4164278 | — | IC50 | - | — | - | |
| CHEMBL4175597 | — | IC50 | - | — | - | |
| CHEMBL4160941 | — | IC50 | - | — | - | |
| CHEMBL4174702 | — | IC50 | - | — | - | |
| CHEMBL4166935 | — | IC50 | - | — | - | |
| CHEMBL4161390 | — | IC50 | - | — | - | |
| CHEMBL4164806 | — | IC50 | - | — | - | |
| CHEMBL4175434 | — | IC50 | - | — | - | |
| CHEMBL4173121 | — | IC50 | - | — | - | |
| CHEMBL4165219 | — | IC50 | - | — | - | |
| CHEMBL4176311 | — | IC50 | - | — | - | |
| CHEMBL4163214 | — | IC50 | - | — | - | |
| CHEMBL4167763 | — | IC50 | - | — | - | |
| CHEMBL4167493 | — | IC50 | - | — | - |