Assay Detail
Binding
CHEMBL4338886
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH2 R140Q mutant (unknown origin) transfected using lentiviral expression system in human U87MG cells assessed as reduction in 2-HG content using alpha-ketoglutarate as substrate after 48 hrs by LC-MS analysis
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], 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 | 12 | 8.05 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4280772 | — | — | 1 | 8.52 |
| CHEMBL4278420 | — | — | 1 | 8.40 |
| CHEMBL4280132 | — | — | 1 | 8.22 |
| CHEMBL4278845 | — | — | 1 | 8.15 |
| CHEMBL4283785 | — | — | 1 | 8.10 |
| CHEMBL4277352 | — | — | 1 | 8.05 |
| CHEMBL4288840 | — | — | 1 | 8.05 |
| CHEMBL4278828 | — | — | 1 | 7.85 |
| CHEMBL4282989 | — | — | 1 | 7.85 |
| CHEMBL4292293 | — | — | 1 | 7.66 |
| CHEMBL4289692 | — | — | 1 | 7.66 |
| CHEMBL4284907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4280772 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4278420 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4280132 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4278845 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4283785 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4277352 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4288840 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4278828 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4282989 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4292293 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4289692 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4284907 | — | IC50 | - | — | - |