Assay Detail
Binding
CHEMBL5368523
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Inhibition of wildtype IDH2 (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 | 5.88 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5433752 | — | — | 1 | 6.76 |
| CHEMBL5394948 | — | — | 1 | 6.60 |
| CHEMBL5397750 | — | — | 1 | 6.48 |
| CHEMBL5406499 | — | — | 1 | 6.39 |
| CHEMBL5422550 | — | — | 1 | 5.95 |
| CHEMBL5416375 | — | — | 1 | 5.63 |
| CHEMBL5401153 | — | — | 1 | 5.63 |
| CHEMBL5410201 | — | — | 1 | 5.43 |
| CHEMBL5406543 | — | — | 1 | 5.30 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 4.58 |
| CHEMBL5437453 | — | — | 1 | - |
| CHEMBL5430339 | — | — | 1 | - |
| CHEMBL5432152 | — | — | 1 | - |
| CHEMBL5405494 | — | — | 1 | - |
| CHEMBL5412348 | — | — | 1 | - |
| CHEMBL5397296 | — | — | 1 | - |
| CHEMBL5411897 | — | — | 1 | - |
| CHEMBL5418738 | — | — | 1 | - |
| CHEMBL5407241 | — | — | 1 | - |
| CHEMBL5429258 | — | — | 1 | - |
| CHEMBL5435491 | — | — | 1 | - |
| CHEMBL5405111 | — | — | 1 | - |
| CHEMBL5400632 | — | — | 1 | - |
| CHEMBL5406596 | — | — | 1 | - |
| CHEMBL5441137 | — | — | 1 | - |
| CHEMBL5437900 | — | — | 1 | - |
| CHEMBL5431662 | — | — | 1 | - |
| CHEMBL5404485 | — | — | 1 | - |
| CHEMBL5428697 | — | — | 1 | - |
| CHEMBL5411497 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5433752 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL5394948 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5397750 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5406499 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL5422550 | — | IC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL5416375 | — | IC50 | = | 2352.0 | nM | 5.63 |
| CHEMBL5401153 | — | IC50 | = | 2321.0 | nM | 5.63 |
| CHEMBL5410201 | — | IC50 | = | 3673.0 | nM | 5.43 |
| CHEMBL5406543 | — | IC50 | = | 5003.0 | nM | 5.30 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 26467.0 | nM | 4.58 |
| CHEMBL5432152 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5431332 | — | IC50 | - | — | - | |
| CHEMBL5405494 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5412348 | — | IC50 | - | — | - | |
| CHEMBL5397296 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5411897 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5418738 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5407241 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5429258 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5425240 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5425277 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5426955 | — | IC50 | - | — | - | |
| CHEMBL5430339 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5437453 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5435491 | — | IC50 | - | — | - | |
| CHEMBL5405111 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5400632 | — | IC50 | - | — | - | |
| CHEMBL5406596 | — | IC50 | - | — | - | |
| CHEMBL5441137 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5437900 | — | IC50 | - | — | - | |
| CHEMBL5431662 | — | IC50 | - | — | - | |
| CHEMBL5404485 | — | IC50 | - | — | - | |
| CHEMBL5428697 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5411497 | — | IC50 | > | 30000.0 | nM | - |