Assay Detail
Binding
CHEMBL4325705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Myc-DDK-tagged IDH1 R132C mutant using alpha-ketoglutarate as substrate preincubated for 15 mins followed by substrate and NADPH addition and measured after 45 mins by diaphorase/resazurin dye based assay
6
Total Activities
6
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
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.52 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4469055 | — | — | 1 | 8.40 |
| CHEMBL4464313 | — | — | 1 | 7.96 |
| CHEMBL4456610 | — | — | 1 | 7.62 |
| CHEMBL4437754 | — | — | 1 | 7.40 |
| CHEMBL4297610 | OLUTASIDENIB | 4.0 | 1 | 6.94 |
| CHEMBL4446657 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4469055 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4464313 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4456610 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4437754 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4297610 | OLUTASIDENIB | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4446657 | — | IC50 | = | 159.0 | nM | 6.80 |