Assay Detail
Binding
CHEMBL5356485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant IDH1 R132H mutant (unknown origin) expressed in Escherichia coli BL21(DE3) pLysS cells using 2OG as substrate assessed as 2OG conversion to 2HG incubated for 60 mins in presence of NADPH by spectrophotometric analysis
13
Total Activities
13
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] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.46 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 8.31 |
| CHEMBL3682093 | — | — | 1 | 8.09 |
| CHEMBL5408932 | — | — | 1 | 7.75 |
| CHEMBL4206033 | BAY1436032 | 1.0 | 1 | 7.75 |
| CHEMBL4565370 | — | — | 1 | 7.70 |
| CHEMBL4279047 | VORASIDENIB | 4.0 | 1 | 7.68 |
| CHEMBL3677053 | — | — | 1 | 7.60 |
| CHEMBL2180727 | — | — | 1 | 7.21 |
| CHEMBL5426446 | — | — | 1 | 7.14 |
| CHEMBL4208002 | — | — | 1 | 5.35 |
| CHEMBL2386126 | — | — | 1 | - |
| CHEMBL3392845 | — | — | 1 | - |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3682093 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5408932 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4206033 | BAY1436032 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4565370 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4279047 | VORASIDENIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3677053 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2180727 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5426446 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4208002 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL2386126 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3392845 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3989908 | ENASIDENIB | IC50 | > | 10000.0 | nM | - |