Assay Detail
Binding
CHEMBL5625323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length N-terminal GST-tagged human IDH1 R132H mutant expressed in Escherichia coli in presence of alpha-KG 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 | 6.16 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5631891 | — | — | 1 | 7.30 |
| CHEMBL5632522 | — | — | 1 | 6.80 |
| CHEMBL5632442 | — | — | 1 | 5.81 |
| CHEMBL5632408 | — | — | 1 | 4.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5631891 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5632522 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5632442 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL5632408 | — | IC50 | = | 19390.0 | nM | 4.71 |