Assay Detail
Binding
CHEMBL4708483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH2 R140Q mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-ketoglutarate and NADPH as substrate preincubated with enzyme for 15 mins followed by substrate addition by fluorescence based assay
36
Total Activities
36
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 design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.22 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4753099 | — | — | 1 | 8.21 |
| CHEMBL4800354 | — | — | 1 | 7.91 |
| CHEMBL4796025 | — | — | 1 | 7.86 |
| CHEMBL4786020 | — | — | 1 | 7.76 |
| CHEMBL4753744 | — | — | 1 | 7.74 |
| CHEMBL4783076 | — | — | 1 | 7.73 |
| CHEMBL4782070 | — | — | 1 | 7.70 |
| CHEMBL4746278 | — | — | 1 | 7.65 |
| CHEMBL4756154 | — | — | 1 | 7.58 |
| CHEMBL4750012 | — | — | 1 | 7.53 |
| CHEMBL4754521 | — | — | 1 | 7.48 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 7.45 |
| CHEMBL4790341 | — | — | 1 | 7.44 |
| CHEMBL4739900 | — | — | 1 | 7.43 |
| CHEMBL4779519 | — | — | 1 | 7.42 |
| CHEMBL4781074 | — | — | 1 | 7.42 |
| CHEMBL4751821 | — | — | 1 | 7.42 |
| CHEMBL4787510 | — | — | 1 | 7.42 |
| CHEMBL4793173 | — | — | 1 | 7.40 |
| CHEMBL4762400 | — | — | 1 | 7.34 |
| CHEMBL4761041 | — | — | 1 | 7.34 |
| CHEMBL4786533 | — | — | 1 | 7.29 |
| CHEMBL4794091 | — | — | 1 | 7.21 |
| CHEMBL4784873 | — | — | 1 | 7.19 |
| CHEMBL4756939 | — | — | 1 | 7.10 |
| CHEMBL4790929 | — | — | 1 | 7.01 |
| CHEMBL4782130 | — | — | 1 | 6.98 |
| CHEMBL3989931 | ENASIDENIB MESYLATE | 4.0 | 1 | 6.91 |
| CHEMBL4793042 | — | — | 1 | 6.88 |
| CHEMBL4748664 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4753099 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4800354 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL4796025 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4786020 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4753744 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4783076 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL4782070 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL4746278 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL4756154 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4750012 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4754521 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL4790341 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4739900 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL4787510 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL4779519 | — | IC50 | = | 37.9 | nM | 7.42 |
| CHEMBL4751821 | — | IC50 | = | 37.6 | nM | 7.42 |
| CHEMBL4781074 | — | IC50 | = | 37.6 | nM | 7.42 |
| CHEMBL4793173 | — | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL4761041 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4762400 | — | IC50 | = | 45.6 | nM | 7.34 |
| CHEMBL4786533 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4794091 | — | IC50 | = | 60.9 | nM | 7.21 |
| CHEMBL4784873 | — | IC50 | = | 64.4 | nM | 7.19 |
| CHEMBL4756939 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL4790929 | — | IC50 | = | 98.2 | nM | 7.01 |
| CHEMBL4782130 | — | IC50 | = | 104.6 | nM | 6.98 |
| CHEMBL3989931 | ENASIDENIB MESYLATE | IC50 | = | 123.6 | nM | 6.91 |
| CHEMBL4793042 | — | IC50 | = | 132.7 | nM | 6.88 |
| CHEMBL4748664 | — | IC50 | = | 182.3 | nM | 6.74 |
| CHEMBL4748497 | — | IC50 | = | 266.7 | nM | 6.57 |
| CHEMBL4762182 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL4788410 | — | IC50 | = | 663.4 | nM | 6.18 |
| CHEMBL4753020 | — | IC50 | = | 683.5 | nM | 6.17 |
| CHEMBL4784579 | — | IC50 | = | 699.0 | nM | 6.16 |
| CHEMBL4744069 | — | IC50 | = | 1241.0 | nM | 5.91 |