Assay Detail
Binding
CHEMBL5356494
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to recombinant IDH1 R132H mutant (unknown origin) expressed in Escherichia coli BL21(DE3) pLysS cells assessed as dissociation constant by NMR analysis
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] 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 |
|---|---|---|---|
| Kd | 7 | 5.37 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3682093 | — | — | 1 | 5.96 |
| CHEMBL4206033 | BAY1436032 | 1.0 | 1 | 5.89 |
| CHEMBL4565370 | — | — | 1 | 5.39 |
| CHEMBL4279047 | VORASIDENIB | 4.0 | 1 | 5.30 |
| CHEMBL2180727 | — | — | 1 | 5.07 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 5.05 |
| CHEMBL3989908 | ENASIDENIB | 4.0 | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3682093 | — | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL4206033 | BAY1436032 | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL4565370 | — | Kd | = | 4100.0 | nM | 5.39 |
| CHEMBL4279047 | VORASIDENIB | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL2180727 | — | Kd | = | 8600.0 | nM | 5.07 |
| CHEMBL3989958 | IVOSIDENIB | Kd | = | 9000.0 | nM | 5.05 |
| CHEMBL3989908 | ENASIDENIB | Kd | = | 12000.0 | nM | 4.92 |