Assay Detail
Binding
CHEMBL4256232
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 2-hydroxyglutarate production by LC-MS/MS analysis
14
Total Activities
14
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
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.42 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4289465 | — | — | 1 | 9.00 |
| CHEMBL4278793 | — | — | 1 | 9.00 |
| CHEMBL4289061 | — | — | 1 | 8.52 |
| CHEMBL4282663 | — | — | 1 | 8.10 |
| CHEMBL4282267 | — | — | 1 | 7.89 |
| CHEMBL4277931 | — | — | 1 | 7.28 |
| CHEMBL4281172 | — | — | 1 | 7.18 |
| CHEMBL4285677 | — | — | 1 | 7.14 |
| CHEMBL4282455 | — | — | 1 | 6.81 |
| CHEMBL4285854 | — | — | 1 | 6.55 |
| CHEMBL4292864 | — | — | 1 | 6.53 |
| CHEMBL4289678 | — | — | 1 | 6.30 |
| CHEMBL4293065 | — | — | 1 | 6.22 |
| CHEMBL4277739 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4289465 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4278793 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4289061 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4282663 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4282267 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4277931 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4281172 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4285677 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4282455 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4285854 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL4292864 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL4289678 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL4293065 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL4277739 | — | IC50 | - | — | - |