Assay Detail
Binding
CHEMBL4135754
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 level after 48 hrs by LC-MS/MS analysis
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 | Intermediate |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.27 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166795 | — | — | 1 | 7.89 |
| CHEMBL4172087 | — | — | 1 | 7.85 |
| CHEMBL4169151 | — | — | 1 | 7.85 |
| CHEMBL3947537 | — | — | 1 | 7.62 |
| CHEMBL4162284 | — | — | 1 | 7.39 |
| CHEMBL4160534 | — | — | 1 | 7.38 |
| CHEMBL4173642 | — | — | 1 | 7.33 |
| CHEMBL4177420 | — | — | 1 | 7.17 |
| CHEMBL4163921 | — | — | 1 | 7.16 |
| CHEMBL3949375 | — | — | 1 | 6.99 |
| CHEMBL4165726 | — | — | 1 | 6.84 |
| CHEMBL4164212 | — | — | 1 | 6.59 |
| CHEMBL4167360 | IDH305 | 2.0 | 1 | 6.50 |
| CHEMBL4170686 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166795 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4172087 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4169151 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3947537 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4162284 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4160534 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4173642 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4177420 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4163921 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3949375 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4165726 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4164212 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL4167360 | IDH305 | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4170686 | — | IC50 | < | 2.0 | nM | - |