Assay Detail
Binding
CHEMBL5625286
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Inhibition of IDH1 R132C mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) cells
10
Total Activities
10
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
Challenges for the development of mutant isocitrate dehydrogenases 1 inhibitors to treat glioma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.89 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633478 | — | — | 1 | 8.30 |
| CHEMBL4651002 | SAFUSIDENIB | 2.0 | 1 | 7.96 |
| CHEMBL5631386 | — | — | 1 | 7.58 |
| CHEMBL4439727 | — | — | 1 | 7.03 |
| CHEMBL5631626 | — | — | 1 | 6.60 |
| CHEMBL4571722 | — | — | 1 | 6.57 |
| CHEMBL5631891 | — | — | 1 | 6.42 |
| CHEMBL5632655 | — | — | 1 | 6.34 |
| CHEMBL5632259 | — | — | 1 | 6.25 |
| CHEMBL5633668 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633478 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4651002 | SAFUSIDENIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5631386 | — | IC50 | = | 26.6 | nM | 7.58 |
| CHEMBL4439727 | — | IC50 | = | 92.4 | nM | 7.03 |
| CHEMBL5631626 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4571722 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL5631891 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5632655 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL5632259 | — | IC50 | = | 568.0 | nM | 6.25 |
| CHEMBL5633668 | — | IC50 | = | 1580.0 | nM | 5.80 |