Assay Detail
Binding
CHEMBL5739027
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biochemical Assay: Compound 1 was not initially reported as having the greatest biochemical potency compared to reports for certain other small molecule inhibitors of mIDH-1. Structurally distinct compounds (e.g., AG-120, AG-881, IDH305, IDH889, GSK321, and Bay1436032) and other certain quinolinone-based compounds were initially reported as having greater in vitro potency in biochemical assays measuring activity against certain mIDH-1 isoforms.
66
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibiting mutant IDH-1
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.27 | 9.00 |
| kon | 22 | - | - |
| k_off | 22 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297610 | OLUTASIDENIB | 4.0 | 9 | 9.00 |
| CHEMBL4215717 | — | — | 3 | 8.32 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 3 | 7.92 |
| CHEMBL4206033 | BAY1436032 | 1.0 | 3 | 7.82 |
| CHEMBL4169151 | — | — | 3 | 7.70 |
| CHEMBL4172087 | — | — | 3 | 7.57 |
| CHEMBL4437754 | — | — | 3 | 7.26 |
| CHEMBL6012264 | — | — | 3 | 7.26 |
| CHEMBL4464313 | — | — | 3 | 7.26 |
| CHEMBL4547257 | — | — | 3 | 7.26 |
| CHEMBL5867546 | — | — | 3 | 7.26 |
| CHEMBL4456162 | — | — | 3 | 6.26 |
| CHEMBL5897105 | — | — | 3 | 6.26 |
| CHEMBL5938174 | — | — | 3 | 6.26 |
| CHEMBL4446598 | — | — | 3 | 6.26 |
| CHEMBL4547484 | — | — | 3 | 6.26 |
| CHEMBL5849539 | — | — | 3 | - |
| CHEMBL4469055 | — | — | 3 | - |
| CHEMBL4456610 | — | — | 3 | - |
| CHEMBL5846537 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297610 | OLUTASIDENIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4215717 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4206033 | BAY1436032 | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4169151 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4297610 | OLUTASIDENIB | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL4172087 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4464313 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4437754 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4547257 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6012264 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5867546 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4547484 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5897105 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4456162 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4446598 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5938174 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4464313 | — | k_off | = | - | s-1 | - |
| CHEMBL4469055 | — | kon | = | - | — | - |
| CHEMBL4469055 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5867546 | — | kon | = | - | — | - |
| CHEMBL4169151 | — | k_off | = | - | s-1 | - |
| CHEMBL4297610 | OLUTASIDENIB | kon | = | - | — | - |
| CHEMBL4297610 | OLUTASIDENIB | k_off | = | - | s-1 | - |
| CHEMBL4297610 | OLUTASIDENIB | IC50 | < | 10.0 | nM | - |
| CHEMBL4297610 | OLUTASIDENIB | kon | = | - | — | - |
| CHEMBL4297610 | OLUTASIDENIB | k_off | = | - | s-1 | - |
| CHEMBL3989958 | IVOSIDENIB | kon | = | - | — | - |
| CHEMBL3989958 | IVOSIDENIB | k_off | = | - | s-1 | - |
| CHEMBL5849539 | — | IC50 | > | 22.0 | nM | - |
| CHEMBL5849539 | — | kon | = | - | — | - |
| CHEMBL5849539 | — | k_off | = | - | s-1 | - |
| CHEMBL4172087 | — | kon | = | - | — | - |
| CHEMBL5867546 | — | k_off | = | - | s-1 | - |
| CHEMBL4437754 | — | k_off | = | - | s-1 | - |
| CHEMBL5938174 | — | kon | = | - | — | - |
| CHEMBL5938174 | — | k_off | = | - | s-1 | - |
| CHEMBL5897105 | — | kon | = | - | — | - |
| CHEMBL5897105 | — | k_off | = | - | s-1 | - |
| CHEMBL5846537 | — | kon | = | - | — | - |
| CHEMBL5846537 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL4437754 | — | kon | = | - | — | - |
| CHEMBL4464313 | — | kon | = | - | — | - |
| CHEMBL4456610 | — | k_off | = | - | s-1 | - |
| CHEMBL4456610 | — | kon | = | - | — | - |
| CHEMBL6012264 | — | kon | = | - | — | - |
| CHEMBL4456610 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL6012264 | — | k_off | = | - | s-1 | - |
| CHEMBL5846537 | — | k_off | = | - | s-1 | - |
| CHEMBL4469055 | — | k_off | = | - | s-1 | - |