Assay Detail
Binding
CHEMBL4180897
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal Strep-tagged IDH1 R132C mutant expressed in Escherichia coli BL21(DE3) using alphaKG as substrate preincubated for 30 mins in presence of NADPH followed by substrate addition by LC-MS/MS analysis
2
Total Activities
2
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
Design, synthesis and biological activity of 3-pyrazine-2-yl-oxazolidin-2-ones as novel, potent and selective inhibitors of mutant isocitrate dehydrogenase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.76 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386126 | — | — | 1 | 6.92 |
| CHEMBL4208002 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386126 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4208002 | — | IC50 | = | 259.0 | nM | 6.59 |