Assay Detail
Binding
CHEMBL4338885
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant in glioma patient-derived human TS603 neurosphere 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] 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 | 12 | 8.88 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4278845 | — | — | 1 | 9.60 |
| CHEMBL4283785 | — | — | 1 | 9.52 |
| CHEMBL4280132 | — | — | 1 | 9.15 |
| CHEMBL4280772 | — | — | 1 | 9.00 |
| CHEMBL4277352 | — | — | 1 | 9.00 |
| CHEMBL4278828 | — | — | 1 | 8.70 |
| CHEMBL4288840 | — | — | 1 | 8.40 |
| CHEMBL4282989 | — | — | 1 | 8.40 |
| CHEMBL4289692 | — | — | 1 | 8.15 |
| CHEMBL4292293 | — | — | 1 | - |
| CHEMBL4284907 | — | — | 1 | - |
| CHEMBL4278420 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4278845 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4283785 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4280132 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4280772 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4277352 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4278828 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4288840 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4282989 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4289692 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4292293 | — | IC50 | - | — | - | |
| CHEMBL4284907 | — | IC50 | - | — | - | |
| CHEMBL4278420 | — | IC50 | - | — | - |