Assay Detail
Binding
CHEMBL4199918
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant (unknown origin) using alphaKG as substrate in presence of NADPH by LC-MS/MS analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.44 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214694 | — | — | 1 | 7.44 |
| CHEMBL4216196 | — | — | 1 | 7.41 |
| CHEMBL4207387 | — | — | 1 | 6.21 |
| CHEMBL3682033 | — | — | 1 | 6.09 |
| CHEMBL3677127 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214694 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4216196 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4207387 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3682033 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3677127 | — | IC50 | = | 8800.0 | nM | 5.06 |