Assay Detail
Binding
CHEMBL4258458
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged recombinant human IDH1 R132H mutant expressed in Escherichia coli Rosetta (DE3) preincubated for 30 mins followed by NADPH/alpha-KG addition and measured after 1 hr
12
Total Activities
12
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
Design, synthesis and biological evaluation of novel 5-hydroxy-2-methyl-4<i>H</i>-pyran-4-one derivatives as antiglioma agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.41 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180727 | — | — | 1 | 7.10 |
| CHEMBL4286032 | — | — | 1 | 4.64 |
| CHEMBL4278116 | — | — | 1 | 4.50 |
| CHEMBL4280797 | — | — | 1 | - |
| CHEMBL4280398 | — | — | 1 | - |
| CHEMBL4291032 | — | — | 1 | - |
| CHEMBL4282653 | — | — | 1 | - |
| CHEMBL4293250 | — | — | 1 | - |
| CHEMBL4294325 | — | — | 1 | - |
| CHEMBL4286444 | — | — | 1 | - |
| CHEMBL4279183 | — | — | 1 | - |
| CHEMBL4289867 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180727 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4286032 | — | IC50 | = | 23100.0 | nM | 4.64 |
| CHEMBL4278116 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4280797 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4280398 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4291032 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4282653 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4293250 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4294325 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4286444 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4279183 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4289867 | — | IC50 | > | 50000.0 | nM | - |