Assay Detail
Binding
CHEMBL5509841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant IDH1 R132H mutant (unknown origin) using alpha-ketoglutarate as substrate incubated for 60 mins in presence of NADPH by fluorescence microplate reader
32
Total Activities
32
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 Novel Dual Inhibitors Targeting Mutant IDH1 and NAMPT for the Treatment of Glioma with IDH1Mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.98 | 7.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5562374 | — | — | 1 | 7.83 |
| CHEMBL5560093 | — | — | 1 | 7.60 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 7.56 |
| CHEMBL5558278 | — | — | 1 | 7.49 |
| CHEMBL5562174 | — | — | 1 | 7.47 |
| CHEMBL5517720 | — | — | 1 | 7.43 |
| CHEMBL5532628 | — | — | 1 | 7.42 |
| CHEMBL3947537 | — | — | 1 | 7.37 |
| CHEMBL5568314 | — | — | 1 | 7.34 |
| CHEMBL5564653 | — | — | 1 | 7.30 |
| CHEMBL5556411 | — | — | 1 | 7.26 |
| CHEMBL5542491 | — | — | 1 | 7.24 |
| CHEMBL5562168 | — | — | 1 | 7.21 |
| CHEMBL5562661 | — | — | 1 | 7.17 |
| CHEMBL5563161 | — | — | 1 | 7.16 |
| CHEMBL5557008 | — | — | 1 | 7.11 |
| CHEMBL5559189 | — | — | 1 | 7.09 |
| CHEMBL5523524 | — | — | 1 | 7.08 |
| CHEMBL5558561 | — | — | 1 | 7.06 |
| CHEMBL5560983 | — | — | 1 | 7.01 |
| CHEMBL5556209 | — | — | 1 | 6.87 |
| CHEMBL5555761 | — | — | 1 | 6.76 |
| CHEMBL5557787 | — | — | 1 | 6.54 |
| CHEMBL5517910 | — | — | 1 | 6.49 |
| CHEMBL5562131 | — | — | 1 | 6.46 |
| CHEMBL5518080 | — | — | 1 | 6.44 |
| CHEMBL5561682 | — | — | 1 | 6.43 |
| CHEMBL5556636 | — | — | 1 | 6.42 |
| CHEMBL5565608 | — | — | 1 | 6.41 |
| CHEMBL5556923 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5562374 | — | IC50 | = | 14.93 | nM | 7.83 |
| CHEMBL5560093 | — | IC50 | = | 25.18 | nM | 7.60 |
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 27.73 | nM | 7.56 |
| CHEMBL5558278 | — | IC50 | = | 32.73 | nM | 7.49 |
| CHEMBL5562174 | — | IC50 | = | 33.96 | nM | 7.47 |
| CHEMBL5517720 | — | IC50 | = | 36.95 | nM | 7.43 |
| CHEMBL5532628 | — | IC50 | = | 37.98 | nM | 7.42 |
| CHEMBL3947537 | — | IC50 | = | 42.51 | nM | 7.37 |
| CHEMBL5568314 | — | IC50 | = | 45.31 | nM | 7.34 |
| CHEMBL5564653 | — | IC50 | = | 49.71 | nM | 7.30 |
| CHEMBL5556411 | — | IC50 | = | 54.6 | nM | 7.26 |
| CHEMBL5542491 | — | IC50 | = | 57.24 | nM | 7.24 |
| CHEMBL5562168 | — | IC50 | = | 61.33 | nM | 7.21 |
| CHEMBL5562661 | — | IC50 | = | 67.06 | nM | 7.17 |
| CHEMBL5563161 | — | IC50 | = | 69.71 | nM | 7.16 |
| CHEMBL5557008 | — | IC50 | = | 78.44 | nM | 7.11 |
| CHEMBL5559189 | — | IC50 | = | 81.73 | nM | 7.09 |
| CHEMBL5523524 | — | IC50 | = | 83.86 | nM | 7.08 |
| CHEMBL5558561 | — | IC50 | = | 87.3 | nM | 7.06 |
| CHEMBL5560983 | — | IC50 | = | 97.3 | nM | 7.01 |
| CHEMBL5556209 | — | IC50 | = | 135.5 | nM | 6.87 |
| CHEMBL5555761 | — | IC50 | = | 175.3 | nM | 6.76 |
| CHEMBL5557787 | — | IC50 | = | 289.4 | nM | 6.54 |
| CHEMBL5517910 | — | IC50 | = | 323.2 | nM | 6.49 |
| CHEMBL5562131 | — | IC50 | = | 345.7 | nM | 6.46 |
| CHEMBL5518080 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL5561682 | — | IC50 | = | 375.4 | nM | 6.43 |
| CHEMBL5556636 | — | IC50 | = | 379.5 | nM | 6.42 |
| CHEMBL5565608 | — | IC50 | = | 392.4 | nM | 6.41 |
| CHEMBL5556923 | — | IC50 | = | 462.7 | nM | 6.33 |
| CHEMBL5557130 | — | IC50 | = | 473.3 | nM | 6.33 |
| CHEMBL5567202 | — | IC50 | = | 1659.0 | nM | 5.78 |