Assay Detail
Binding
CHEMBL2188262
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Inhibition of IDH1 R132H mutant using alpha-ketoglutarate as substrate after 60 mins by resazurin-based fluorimetric analysis
36
Total Activities
36
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 the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.41 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180739 | — | — | 1 | 7.30 |
| CHEMBL2180730 | — | — | 1 | 7.30 |
| CHEMBL2180748 | — | — | 1 | 7.22 |
| CHEMBL2180740 | — | — | 1 | 7.22 |
| CHEMBL2180393 | — | — | 1 | 7.22 |
| CHEMBL2180727 | — | — | 1 | 7.16 |
| CHEMBL2180729 | — | — | 1 | 7.16 |
| CHEMBL2180747 | — | — | 1 | 7.10 |
| CHEMBL2180394 | — | — | 1 | 7.10 |
| CHEMBL2180728 | — | — | 1 | 7.10 |
| CHEMBL2180746 | — | — | 1 | 7.05 |
| CHEMBL2180738 | — | — | 1 | 7.00 |
| CHEMBL2180400 | — | — | 1 | 6.85 |
| CHEMBL2180398 | — | — | 1 | 6.85 |
| CHEMBL2180744 | — | — | 1 | 6.72 |
| CHEMBL2180396 | — | — | 1 | 6.62 |
| CHEMBL2180731 | — | — | 1 | 6.54 |
| CHEMBL2180399 | — | — | 1 | 6.38 |
| CHEMBL2180745 | — | — | 1 | 6.35 |
| CHEMBL2180734 | — | — | 1 | 6.24 |
| CHEMBL2180736 | — | — | 1 | 6.19 |
| CHEMBL2180732 | — | — | 1 | 6.07 |
| CHEMBL2180742 | — | — | 1 | 6.05 |
| CHEMBL2180741 | — | — | 1 | 5.96 |
| CHEMBL2180392 | — | — | 1 | 5.90 |
| CHEMBL2180750 | — | — | 1 | 5.85 |
| CHEMBL2180395 | — | — | 1 | 5.79 |
| CHEMBL2180735 | — | — | 1 | 5.75 |
| CHEMBL2180733 | — | — | 1 | 5.54 |
| CHEMBL2180751 | — | — | 1 | 5.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180739 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2180730 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2180740 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2180393 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2180748 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2180727 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2180729 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2180747 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2180394 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2180728 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2180746 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2180738 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2180400 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2180398 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2180744 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2180396 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2180731 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2180399 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2180745 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2180734 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2180736 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2180732 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL2180742 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2180741 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2180392 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL2180750 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2180395 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL2180735 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2180733 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL2180751 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2180397 | — | IC50 | = | 5640.0 | nM | 5.25 |
| CHEMBL2180743 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL2180737 | — | IC50 | = | 53100.0 | nM | 4.28 |
| CHEMBL2180753 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2180752 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2180749 | — | IC50 | > | 11000.0 | nM | - |