Assay Detail
Binding
CHEMBL5261222
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant expressed in human HCT-116 cells assessed as effect on intracellular 2-HG level incubated for 48 hrs by LC/MS/MS analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Isocitrate dehydrogenase [NADP] cytoplasmic (CHEMBL2007625) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.42 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169151 | — | — | 1 | 7.85 |
| CHEMBL3677013 | — | — | 1 | 7.66 |
| CHEMBL5273829 | — | — | 1 | 7.05 |
| CHEMBL5289157 | — | — | 1 | 6.80 |
| CHEMBL3672144 | — | — | 1 | 6.80 |
| CHEMBL5269195 | — | — | 1 | 6.77 |
| CHEMBL4216196 | — | — | 1 | 6.70 |
| CHEMBL3672192 | — | — | 1 | 6.48 |
| CHEMBL3639710 | — | — | 1 | 6.46 |
| CHEMBL5267963 | — | — | 1 | 6.38 |
| CHEMBL3672163 | — | — | 1 | 6.37 |
| CHEMBL5277001 | — | — | 1 | 6.30 |
| CHEMBL3672183 | — | — | 1 | 6.28 |
| CHEMBL3672097 | — | — | 1 | 6.18 |
| CHEMBL3677089 | — | — | 1 | 6.16 |
| CHEMBL3672135 | — | — | 1 | 6.06 |
| CHEMBL3672129 | — | — | 1 | 5.96 |
| CHEMBL3672198 | — | — | 1 | 5.93 |
| CHEMBL5273919 | — | — | 1 | 5.87 |
| CHEMBL5281535 | — | — | 1 | 5.60 |
| CHEMBL3639759 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169151 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3677013 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5273829 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5289157 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3672144 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5269195 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4216196 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3672192 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3639710 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5267963 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3672163 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5277001 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3672183 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3672097 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3677089 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3672135 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3672129 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3672198 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL5273919 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL5281535 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3639759 | — | IC50 | = | 7900.0 | nM | 5.10 |