Assay Detail
Binding
CHEMBL4628667
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH2 R172K mutant (unknown origin)
7
Total Activities
7
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
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.84 | 5.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 5.97 |
| CHEMBL3392845 | — | — | 1 | 4.98 |
| CHEMBL4639434 | — | — | 1 | 4.29 |
| CHEMBL4646777 | — | — | 1 | 4.10 |
| CHEMBL4634103 | — | — | 1 | - |
| CHEMBL4643441 | — | — | 1 | - |
| CHEMBL2180727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989908 | ENASIDENIB | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3392845 | — | IC50 | = | 10390.0 | nM | 4.98 |
| CHEMBL4639434 | — | IC50 | = | 51800.0 | nM | 4.29 |
| CHEMBL4646777 | — | IC50 | = | 78800.0 | nM | 4.10 |
| CHEMBL4634103 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4643441 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2180727 | — | IC50 | > | 100000.0 | nM | - |