Assay Detail
Binding
CHEMBL5625321
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal 6His-tagged IDH1 R132C mutant expressed in Escherichia coli Rosetta2 (DE3) in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
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 | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.24 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215717 | — | — | 1 | 8.42 |
| CHEMBL5633996 | — | — | 1 | 8.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215717 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5633996 | — | IC50 | = | 8.8 | nM | 8.06 |