Assay Detail
Binding
CHEMBL2188256
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Inhibition of IDH1 R132C mutant using alpha-ketoglutarate as substrate after 60 mins by resazurin-based fluorimetric analysis
8
Total Activities
8
Compounds Tested
1
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
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 | 7.31 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180740 | — | — | 1 | 7.52 |
| CHEMBL2180730 | — | — | 1 | 7.52 |
| CHEMBL2180729 | — | — | 1 | 7.40 |
| CHEMBL2180728 | — | — | 1 | 7.40 |
| CHEMBL2180739 | — | — | 1 | 7.30 |
| CHEMBL2180746 | — | — | 1 | 7.30 |
| CHEMBL2180738 | — | — | 1 | 7.22 |
| CHEMBL2180727 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180740 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2180730 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2180729 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2180728 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2180739 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2180746 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2180738 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2180727 | — | IC50 | = | 160.0 | nM | 6.80 |