Assay Detail
Binding
CHEMBL4338881
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length C-terminal His8 tagged IDH1 R132H mutant (1 to 414 residues) (unknown origin) homodimer expressed in Escherichia coli BE3 cells assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate after 60 mins by Diaphorase/Resazurin dye based fluorescence assay
3
Total Activities
3
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
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 | 3 | 6.58 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4278828 | — | — | 1 | 7.32 |
| CHEMBL4448857 | — | — | 1 | 7.11 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4278828 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4448857 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 4950.0 | nM | 5.30 |