Assay Detail
Binding
CHEMBL2188258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant expressed in human U87 cells assessed as inhibition of 2-hydroxyglutarate production after 48 hrs by LC/MS analysis
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.60 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180727 | — | — | 1 | 7.16 |
| CHEMBL2180730 | — | — | 1 | 6.72 |
| CHEMBL2180739 | — | — | 1 | 6.68 |
| CHEMBL2180728 | — | — | 1 | 6.62 |
| CHEMBL2180738 | — | — | 1 | 6.54 |
| CHEMBL2180740 | — | — | 1 | 6.44 |
| CHEMBL2180729 | — | — | 1 | 6.43 |
| CHEMBL2180746 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180727 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2180730 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2180739 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2180728 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2180738 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2180740 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2180729 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2180746 | — | IC50 | = | 580.0 | nM | 6.24 |