Assay Detail
Binding
CHEMBL4332272
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-fused IDH1 R132L mutant expressed in Escherichia coli using alpha-ketoglutarate as substrate preincubated for 15 mins followed by substrate addition
7
Total Activities
7
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
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.60 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180727 | — | — | 1 | 6.73 |
| CHEMBL4476190 | — | — | 1 | 6.72 |
| CHEMBL4556914 | — | — | 1 | 6.72 |
| CHEMBL4465287 | — | — | 1 | 6.61 |
| CHEMBL4514241 | — | — | 1 | 6.51 |
| CHEMBL4469450 | — | — | 1 | 6.51 |
| CHEMBL4559482 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180727 | — | IC50 | = | 186.1 | nM | 6.73 |
| CHEMBL4476190 | — | IC50 | = | 189.1 | nM | 6.72 |
| CHEMBL4556914 | — | IC50 | = | 191.5 | nM | 6.72 |
| CHEMBL4465287 | — | IC50 | = | 246.4 | nM | 6.61 |
| CHEMBL4514241 | — | IC50 | = | 307.1 | nM | 6.51 |
| CHEMBL4469450 | — | IC50 | = | 310.6 | nM | 6.51 |
| CHEMBL4559482 | — | IC50 | = | 398.2 | nM | 6.40 |