Assay Detail
Binding
CHEMBL5608770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Sterp-II tagged recombinant human full length IDH1 R132H mutant extracted from Escherichia coli using alpha-ketoglutarate as substrate assessed as reduction in 2-HG level incubated for 90 mins by fluorescent reader
1
Total Activities
1
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
Discovery of novel natural-product-derived mutant isocitrate dehydrogenases 1 inhibitors: Structure-based virtual screening, biological evaluation and structure-activity relationship study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 7.82 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4206033 | BAY1436032 | 1.0 | 1 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4206033 | BAY1436032 | IC50 | = | 15.0 | nM | 7.82 |