Assay Detail
Binding
CHEMBL5368526
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH2 R140Q mutant (unknown origin) expressed in human TF-1 cells assessed as inhibition of D2HG production incubated for 3 days by UHPL HRMS analysis
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | TF-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP], mitochondrial (CHEMBL3991501) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2<sup>R140Q</sup> Inhibitors with High Selectivity and Reduced hERG Inhibitory Activity for the Treatment of Acute Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.27 | 8.00 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5441137 | — | — | 2 | 8.00 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 7.96 |
| CHEMBL5428697 | — | — | 1 | 7.68 |
| CHEMBL5418738 | — | — | 1 | 7.28 |
| CHEMBL5432152 | — | — | 1 | 7.01 |
| CHEMBL5397296 | — | — | 1 | 6.94 |
| CHEMBL5405494 | — | — | 1 | 6.70 |
| CHEMBL5430339 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5441137 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5428697 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5418738 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5432152 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5397296 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL5405494 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL5430339 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5441137 | — | Inhibition | - | % | - |