Assay Detail
Binding
CHEMBL4325706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Myc-DDK-tagged IDH1 R132H 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
14
Total Activities
14
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 | 14 | 7.13 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456610 | — | — | 1 | 8.10 |
| CHEMBL4469055 | — | — | 1 | 8.10 |
| CHEMBL4437754 | — | — | 1 | 7.96 |
| CHEMBL4464313 | — | — | 1 | 7.96 |
| CHEMBL4297610 | OLUTASIDENIB | 4.0 | 1 | 7.67 |
| CHEMBL4446657 | — | — | 1 | 7.60 |
| CHEMBL4547257 | — | — | 1 | 7.39 |
| CHEMBL4454572 | — | — | 1 | 7.19 |
| CHEMBL4461178 | — | — | 1 | 6.80 |
| CHEMBL4547484 | — | — | 1 | 6.65 |
| CHEMBL4446598 | — | — | 1 | 6.45 |
| CHEMBL4456162 | — | — | 1 | 6.16 |
| CHEMBL4533443 | — | — | 1 | 4.60 |
| CHEMBL4532955 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456610 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4469055 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4437754 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4464313 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4297610 | OLUTASIDENIB | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL4446657 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4547257 | — | IC50 | = | 40.3 | nM | 7.39 |
| CHEMBL4454572 | — | IC50 | = | 64.7 | nM | 7.19 |
| CHEMBL4461178 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4547484 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4446598 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL4456162 | — | IC50 | = | 694.0 | nM | 6.16 |
| CHEMBL4533443 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4532955 | — | IC50 | > | 25000.0 | nM | - |