Assay Detail
Binding
CHEMBL4325709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant in human HCT116 cells assessed as reduction in 2-HG levels after 24 hrs by RapidFire high-throughput mass spectrometry assay
7
Total Activities
6
Compounds Tested
2
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 | 8.11 | 8.70 |
| fIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456610 | — | — | 1 | 8.70 |
| CHEMBL4437754 | — | — | 1 | 8.40 |
| CHEMBL4297610 | OLUTASIDENIB | 4.0 | 2 | 7.68 |
| CHEMBL4446657 | — | — | 1 | 7.66 |
| CHEMBL4464313 | — | — | 1 | - |
| CHEMBL4469055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456610 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4437754 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4297610 | OLUTASIDENIB | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4446657 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4297610 | OLUTASIDENIB | fIC50 | = | 37.0 | nM | - |
| CHEMBL4464313 | — | IC50 | < | 2.0 | nM | - |
| CHEMBL4469055 | — | IC50 | < | 2.0 | nM | - |