Assay Detail
Binding
CHEMBL5625322
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant IDH1 R132H mutant expressed in Escherichia coli BL21 (DE3) cells in presence of alpha-ketoglutarate and NADPH by fluorescence based biochemical assay
4
Total Activities
4
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 | 4 | 7.64 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215717 | — | — | 1 | 8.54 |
| CHEMBL5632690 | — | — | 1 | 7.96 |
| CHEMBL5633996 | — | — | 1 | 7.82 |
| CHEMBL5631935 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215717 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5632690 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5633996 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL5631935 | — | IC50 | = | 590.0 | nM | 6.23 |