Assay Detail
Binding
CHEMBL4135748
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Inhibition of IDH1 R132H mutant (unknown origin) using alpha-ketoglutarate as substrate 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 | 7.43 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170686 | — | — | 1 | 8.40 |
| CHEMBL4172087 | — | — | 1 | 7.89 |
| CHEMBL4166795 | — | — | 1 | 7.82 |
| CHEMBL3947537 | — | — | 1 | 7.75 |
| CHEMBL4169151 | — | — | 1 | 7.70 |
| CHEMBL4163921 | — | — | 1 | 7.55 |
| CHEMBL3949375 | — | — | 1 | 7.48 |
| CHEMBL4160534 | — | — | 1 | 7.46 |
| CHEMBL4173642 | — | — | 1 | 7.21 |
| CHEMBL4167360 | IDH305 | 2.0 | 1 | 7.14 |
| CHEMBL4162284 | — | — | 1 | 7.11 |
| CHEMBL4177420 | — | — | 1 | 7.08 |
| CHEMBL4164212 | — | — | 1 | 6.94 |
| CHEMBL4165726 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170686 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4172087 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4166795 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3947537 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4169151 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4163921 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3949375 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4160534 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4173642 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4167360 | IDH305 | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4162284 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4177420 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4164212 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4165726 | — | IC50 | = | 339.0 | nM | 6.47 |