Assay Detail
Binding
CHEMBL5625285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human IDH1 R132H mutant
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.73 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4651002 | SAFUSIDENIB | 2.0 | 1 | 8.08 |
| CHEMBL3947537 | — | — | 1 | 7.75 |
| CHEMBL3677013 | — | — | 1 | 7.66 |
| CHEMBL5632211 | — | — | 1 | 7.62 |
| CHEMBL4472519 | — | — | 1 | 7.14 |
| CHEMBL5632778 | — | — | 1 | 6.57 |
| CHEMBL5631659 | — | — | 1 | 6.47 |
| CHEMBL5632619 | — | — | 1 | 6.45 |
| CHEMBL5632881 | — | — | 1 | 6.38 |
| CHEMBL5633550 | — | — | 1 | 5.78 |
| CHEMBL139702 | LICOAGROCHACONE A | — | 1 | 4.11 |
| CHEMBL5633568 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4651002 | SAFUSIDENIB | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3947537 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3677013 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5632211 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL4472519 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5632778 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL5631659 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL5632619 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL5632881 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL5633550 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL139702 | LICOAGROCHACONE A | IC50 | = | 76870.0 | nM | 4.11 |
| CHEMBL5633568 | — | IC50 | > | 50000.0 | nM | - |