Assay Detail
Binding
CHEMBL4409430
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-HG production incubated with compound for 48 hrs by D2HG assay kit based fluorescence assay
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
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.57 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4475715 | — | — | 1 | 7.92 |
| CHEMBL4444067 | — | — | 1 | 7.90 |
| CHEMBL4568616 | — | — | 1 | 7.80 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 7.59 |
| CHEMBL3947537 | — | — | 1 | 7.28 |
| CHEMBL4467991 | — | — | 1 | 7.27 |
| CHEMBL4469477 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4475715 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4444067 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL4568616 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL3947537 | — | IC50 | = | 52.7 | nM | 7.28 |
| CHEMBL4467991 | — | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL4469477 | — | IC50 | = | 60.3 | nM | 7.22 |