Assay Detail
Binding
CHEMBL3389009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132C mutant in human HT1080 cells assessed as reduction in D2HG production incubated for 48 hrs by HPLC-MS method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-1080 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.47 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3343444 | — | — | 1 | 5.96 |
| CHEMBL3343462 | — | — | 1 | 5.96 |
| CHEMBL2386125 | — | — | 1 | 5.62 |
| CHEMBL3343463 | — | — | 1 | 5.50 |
| CHEMBL3343445 | — | — | 1 | 5.42 |
| CHEMBL3343464 | — | — | 1 | 5.20 |
| CHEMBL2386128 | — | — | 1 | 5.07 |
| CHEMBL2386127 | — | — | 1 | 5.01 |
| CHEMBL3343434 | — | — | 1 | - |
| CHEMBL2386126 | — | — | 1 | - |
| CHEMBL2386129 | — | — | 1 | - |
| CHEMBL3343439 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3343444 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3343462 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2386125 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3343463 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3343445 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3343464 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL2386128 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2386127 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL3343434 | — | IC50 | - | — | - | |
| CHEMBL2386126 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL2386129 | — | IC50 | - | — | - | |
| CHEMBL3343439 | — | IC50 | > | 30000.0 | nM | - |