Assay Detail
Binding
CHEMBL4812397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal NanoLuc 86b-tagged IDH1 R132H (unknown origin) expressed in HEK293T cells assessed as increase in thermal stability by measuring Nano-luciferase activity at 56 degC for 3.5 min by CETSA
3
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of 2<i>H</i>-1λ<sup>2</sup>-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 7.41 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 7.90 |
| CHEMBL4448475 | — | — | 2 | 7.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | EC50 | = | 12.47 | nM | 7.90 |
| CHEMBL4448475 | — | EC50 | = | 18.02 | nM | 7.74 |
| CHEMBL4448475 | — | EC50 | = | 250.22 | nM | 6.60 |