Assay Detail
Binding
CHEMBL4199919
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant (unknown origin) expressed in HCT116 cells assessed as reduction in 2-HG levels after 48 hrs by LC-MS/MS analysis
11
Total Activities
11
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 | 11 | 7.49 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3986241 | — | — | 1 | 8.40 |
| CHEMBL4216510 | — | — | 1 | 7.89 |
| CHEMBL4208648 | — | — | 1 | 7.82 |
| CHEMBL3909586 | — | — | 1 | 7.82 |
| CHEMBL3959391 | — | — | 1 | 7.66 |
| CHEMBL3894881 | — | — | 1 | 7.62 |
| CHEMBL3953686 | — | — | 1 | 7.52 |
| CHEMBL4216983 | — | — | 1 | 7.41 |
| CHEMBL4217038 | — | — | 1 | 7.33 |
| CHEMBL4114410 | — | — | 1 | 6.62 |
| CHEMBL4212061 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3986241 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4216510 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4208648 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3909586 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3959391 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3894881 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3953686 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4216983 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4217038 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4114410 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4212061 | — | IC50 | = | 560.0 | nM | 6.25 |