Assay Detail
Binding
CHEMBL5368521
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Inhibition of IDH2 R140Q mutant (unknown origin) using alpha-ketoglutarate as substrate incubated for 16 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 | 6.87 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5405494 | — | — | 1 | 8.15 |
| CHEMBL5428697 | — | — | 1 | 8.10 |
| CHEMBL5430339 | — | — | 1 | 8.05 |
| CHEMBL5397750 | — | — | 1 | 7.64 |
| CHEMBL5433752 | — | — | 1 | 7.62 |
| CHEMBL5410201 | — | — | 1 | 7.60 |
| CHEMBL5441137 | — | — | 1 | 7.54 |
| CHEMBL5432152 | — | — | 1 | 7.51 |
| CHEMBL5406499 | — | — | 1 | 7.50 |
| CHEMBL5401153 | — | — | 1 | 7.43 |
| CHEMBL5418738 | — | — | 1 | 7.42 |
| CHEMBL5394948 | — | — | 1 | 7.28 |
| CHEMBL5406543 | — | — | 1 | 7.25 |
| CHEMBL5422550 | — | — | 1 | 7.18 |
| CHEMBL5407241 | — | — | 1 | 7.15 |
| CHEMBL5397296 | — | — | 1 | 7.09 |
| CHEMBL5429258 | — | — | 1 | 6.98 |
| CHEMBL5411897 | — | — | 1 | 6.80 |
| CHEMBL5405111 | — | — | 1 | 6.80 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 6.75 |
| CHEMBL5416375 | — | — | 1 | 6.71 |
| CHEMBL5425240 | — | — | 1 | 6.64 |
| CHEMBL5437453 | — | — | 1 | 6.54 |
| CHEMBL5425277 | — | — | 1 | 6.43 |
| CHEMBL5411497 | — | — | 1 | 6.37 |
| CHEMBL5412348 | — | — | 1 | 6.31 |
| CHEMBL5406596 | — | — | 1 | 6.04 |
| CHEMBL5437900 | — | — | 1 | 6.00 |
| CHEMBL5431662 | — | — | 1 | 5.95 |
| CHEMBL5431332 | — | — | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5405494 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5428697 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5430339 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5397750 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5433752 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5410201 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5441137 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5432152 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5406499 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5401153 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5418738 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5394948 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5406543 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5422550 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5407241 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5397296 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5429258 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5411897 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5405111 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL5416375 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5425240 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL5437453 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL5425277 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL5411497 | — | IC50 | = | 423.0 | nM | 6.37 |
| CHEMBL5412348 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL5406596 | — | IC50 | = | 909.0 | nM | 6.04 |
| CHEMBL5437900 | — | IC50 | = | 989.0 | nM | 6.00 |
| CHEMBL5431662 | — | IC50 | = | 1118.0 | nM | 5.95 |
| CHEMBL5431332 | — | IC50 | = | 1122.0 | nM | 5.95 |
| CHEMBL5435491 | — | IC50 | = | 1453.0 | nM | 5.84 |
| CHEMBL5404485 | — | IC50 | = | 1656.0 | nM | 5.78 |
| CHEMBL5400632 | — | IC50 | = | 1751.0 | nM | 5.76 |
| CHEMBL5426955 | — | IC50 | = | 5667.0 | nM | 5.25 |