Assay Detail
Binding
CHEMBL4338883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length C-terminal His6 tagged IDH2 R140Q mutant (1 to 452 residues) (unknown origin) homodimer expressed in Sf9 cells assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate preincubated for 16 hrs followed by substrate addition and measured after 1 hr by Diaphorase/Resazurin dye based fluorescence assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP], mitochondrial (CHEMBL3991501) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.64 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 8.05 |
| CHEMBL4292293 | — | — | 1 | 7.89 |
| CHEMBL4280772 | — | — | 1 | 7.80 |
| CHEMBL4448857 | — | — | 1 | 7.72 |
| CHEMBL4278828 | — | — | 1 | 7.66 |
| CHEMBL4284907 | — | — | 1 | 7.34 |
| CHEMBL4288840 | — | — | 1 | 7.04 |
| CHEMBL4277352 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4292293 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4280772 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4448857 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4278828 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4284907 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4288840 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4277352 | — | IC50 | - | — | - |