Assay Detail
Binding
CHEMBL4338879
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) expressed in Escherichia coli BE3 cells/wild type IDH1 (unknown origin) heterodimer assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate after 60 mins by Diaphorase/Resazurin dye based fluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 23 | 7.34 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4278845 | — | — | 1 | 9.22 |
| CHEMBL4278828 | — | — | 1 | 8.22 |
| CHEMBL4282989 | — | — | 1 | 8.22 |
| CHEMBL4280132 | — | — | 1 | 8.22 |
| CHEMBL4277352 | — | — | 1 | 8.22 |
| CHEMBL4283785 | — | — | 1 | 8.15 |
| CHEMBL4280772 | — | — | 1 | 8.05 |
| CHEMBL4278420 | — | — | 1 | 8.05 |
| CHEMBL4448857 | — | — | 1 | 7.70 |
| CHEMBL4289692 | — | — | 1 | 7.66 |
| CHEMBL4288840 | — | — | 1 | 7.57 |
| CHEMBL4284907 | — | — | 1 | 7.22 |
| CHEMBL4292293 | — | — | 1 | 7.08 |
| CHEMBL4292856 | — | — | 1 | 6.85 |
| CHEMBL4285495 | — | — | 1 | 6.73 |
| CHEMBL4276904 | — | — | 1 | 6.70 |
| CHEMBL4293274 | — | — | 1 | 6.41 |
| CHEMBL4289685 | — | — | 1 | 6.17 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 6.17 |
| CHEMBL4284596 | — | — | 1 | 5.80 |
| CHEMBL4277032 | — | — | 1 | 5.76 |
| CHEMBL4473884 | — | — | 1 | - |
| CHEMBL4560615 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4278845 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4278828 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4282989 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4280132 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4277352 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4283785 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4280772 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4278420 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4448857 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4289692 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4288840 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4284907 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4292293 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4292856 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4285495 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4276904 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL4293274 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL4289685 | — | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL4284596 | — | IC50 | = | 1566.0 | nM | 5.80 |
| CHEMBL4277032 | — | IC50 | = | 1749.0 | nM | 5.76 |
| CHEMBL4473884 | — | IC50 | - | — | - | |
| CHEMBL4560615 | — | IC50 | - | — | - |