Assay Detail
Binding
CHEMBL4835353
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Inhibition of human TRPM2 expressed in HEK293T cells assessed as blocked of ADPR-activated current by whole cell patch clamp electrophysiology
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.87 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878260 | — | — | 1 | 7.89 |
| CHEMBL487005 | SCALARADIAL | — | 1 | 6.68 |
| CHEMBL4863360 | — | — | 1 | 6.40 |
| CHEMBL4864346 | — | — | 1 | 6.39 |
| CHEMBL4856222 | — | — | 1 | 6.33 |
| CHEMBL4863549 | — | — | 1 | 6.10 |
| CHEMBL4849043 | — | — | 1 | 6.08 |
| CHEMBL4856093 | — | — | 1 | 6.01 |
| CHEMBL169233 | — | — | 1 | 5.92 |
| CHEMBL173443 | — | — | 1 | 5.77 |
| CHEMBL176974 | — | — | 1 | 5.59 |
| CHEMBL808 | ECONAZOLE | 4.0 | 1 | 5.52 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 1 | 5.52 |
| CHEMBL4176916 | — | — | 1 | 5.43 |
| CHEMBL23588 | FLUFENAMIC ACID | 2.0 | 1 | 4.16 |
| CHEMBL23479 | — | — | 1 | 4.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878260 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL487005 | SCALARADIAL | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4863360 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL4864346 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4856222 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL4863549 | — | IC50 | = | 788.0 | nM | 6.10 |
| CHEMBL4849043 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4856093 | — | IC50 | = | 987.0 | nM | 6.01 |
| CHEMBL169233 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL173443 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL176974 | — | IC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL808 | ECONAZOLE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4176916 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL23588 | FLUFENAMIC ACID | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL23479 | — | IC50 | = | 76000.0 | nM | 4.12 |