Assay Detail
Functional
CHEMBL5509853
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Antiproliferative activity against human U-87 MG cells harboring IDH1 R132H mutant assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.02 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3947537 | — | — | 1 | 6.36 |
| CHEMBL5562174 | — | — | 1 | 6.33 |
| CHEMBL566757 | DAPORINAD | 2.0 | 1 | 6.01 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 5.99 |
| CHEMBL5517720 | — | — | 1 | 5.93 |
| CHEMBL5523524 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3947537 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5562174 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL566757 | DAPORINAD | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5517720 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL5523524 | — | IC50 | = | 3260.0 | nM | 5.49 |