Assay Detail
Binding
CHEMBL5368522
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH2 R140Q mutant (unknown origin) using alpha-ketoglutarate as substrate incubated for 1 hrs in the presence of NADPH by absorbance based plate reader analysis
34
Total Activities
34
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], 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 | 34 | 6.45 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5430339 | — | — | 1 | 7.58 |
| CHEMBL5405494 | — | — | 1 | 7.54 |
| CHEMBL5428697 | — | — | 1 | 7.43 |
| CHEMBL5401153 | — | — | 1 | 7.33 |
| CHEMBL5406499 | — | — | 1 | 7.27 |
| CHEMBL5410201 | — | — | 1 | 7.09 |
| CHEMBL5397750 | — | — | 1 | 7.06 |
| CHEMBL5418738 | — | — | 1 | 7.03 |
| CHEMBL5432152 | — | — | 1 | 6.90 |
| CHEMBL5407241 | — | — | 1 | 6.83 |
| CHEMBL5433752 | — | — | 1 | 6.81 |
| CHEMBL5429258 | — | — | 1 | 6.74 |
| CHEMBL5441137 | — | — | 1 | 6.69 |
| CHEMBL5406543 | — | — | 1 | 6.66 |
| CHEMBL5397296 | — | — | 1 | 6.60 |
| CHEMBL5437453 | — | — | 1 | 6.54 |
| CHEMBL5411897 | — | — | 1 | 6.53 |
| CHEMBL5394948 | — | — | 1 | 6.53 |
| CHEMBL5422550 | — | — | 1 | 6.50 |
| CHEMBL5405111 | — | — | 1 | 6.43 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 6.36 |
| CHEMBL5431662 | — | — | 1 | 6.11 |
| CHEMBL5411497 | — | — | 1 | 6.08 |
| CHEMBL5425240 | — | — | 1 | 6.07 |
| CHEMBL5416375 | — | — | 1 | 6.04 |
| CHEMBL5406596 | — | — | 1 | 5.98 |
| CHEMBL5437900 | — | — | 1 | 5.94 |
| CHEMBL5412348 | — | — | 1 | 5.91 |
| CHEMBL5404485 | — | — | 1 | 5.74 |
| CHEMBL5425277 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5430339 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5405494 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5428697 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5401153 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5406499 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5410201 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5397750 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5418738 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5432152 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5407241 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL5433752 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5429258 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL5441137 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5406543 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL5397296 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL5437453 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL5394948 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL5411897 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL5422550 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5405111 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL5431662 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL5411497 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL5425240 | — | IC50 | = | 848.0 | nM | 6.07 |
| CHEMBL5416375 | — | IC50 | = | 921.0 | nM | 6.04 |
| CHEMBL5406596 | — | IC50 | = | 1037.0 | nM | 5.98 |
| CHEMBL5437900 | — | IC50 | = | 1152.0 | nM | 5.94 |
| CHEMBL5412348 | — | IC50 | = | 1232.0 | nM | 5.91 |
| CHEMBL5404485 | — | IC50 | = | 1821.0 | nM | 5.74 |
| CHEMBL5425277 | — | IC50 | = | 1855.0 | nM | 5.73 |
| CHEMBL5400632 | — | IC50 | = | 1961.0 | nM | 5.71 |
| CHEMBL5431332 | — | IC50 | = | 1931.0 | nM | 5.71 |
| CHEMBL5435491 | — | IC50 | = | 2148.0 | nM | 5.67 |
| CHEMBL5426955 | — | IC50 | = | 50431.0 | nM | 4.30 |