Assay Detail
Binding
CHEMBL5371973
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Inhibition of IDH1 R132H mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as NADPH consumption using alpha-KG as substrate measured after 60 mins
40
Total Activities
40
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
Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.53 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 8.35 |
| CHEMBL5425749 | — | — | 1 | 8.33 |
| CHEMBL5420050 | — | — | 1 | 8.23 |
| CHEMBL5440722 | — | — | 1 | 7.38 |
| CHEMBL5436549 | — | — | 1 | 7.32 |
| CHEMBL5399782 | — | — | 1 | 7.26 |
| CHEMBL5403346 | — | — | 1 | 7.11 |
| CHEMBL5432595 | — | — | 1 | 7.06 |
| CHEMBL5426656 | — | — | 1 | 7.06 |
| CHEMBL5395437 | — | — | 1 | 7.06 |
| CHEMBL5431953 | — | — | 1 | 6.92 |
| CHEMBL5425321 | — | — | 1 | 6.84 |
| CHEMBL5401096 | — | — | 1 | 6.82 |
| CHEMBL5395971 | — | — | 1 | 6.81 |
| CHEMBL5430621 | — | — | 1 | 6.79 |
| CHEMBL5395826 | — | — | 1 | 6.73 |
| CHEMBL5402222 | — | — | 1 | 6.72 |
| CHEMBL5410097 | — | — | 1 | 6.70 |
| CHEMBL5429617 | — | — | 1 | 6.69 |
| CHEMBL5394135 | — | — | 1 | 6.61 |
| CHEMBL5406779 | — | — | 1 | 6.36 |
| CHEMBL5429295 | — | — | 1 | 6.29 |
| CHEMBL5436810 | — | — | 1 | 6.27 |
| CHEMBL5398072 | — | — | 1 | 6.26 |
| CHEMBL5436629 | — | — | 1 | 6.23 |
| CHEMBL5435681 | — | — | 1 | 6.20 |
| CHEMBL5422753 | — | — | 1 | 6.17 |
| CHEMBL5410611 | — | — | 1 | 6.13 |
| CHEMBL5407884 | — | — | 1 | 6.05 |
| CHEMBL5413084 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5425749 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5420050 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5440722 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5436549 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5399782 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5403346 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5432595 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5426656 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5395437 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5431953 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5425321 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5401096 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5395971 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5430621 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5395826 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL5402222 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5410097 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL5429617 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL5394135 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL5406779 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5429295 | — | IC50 | = | 516.0 | nM | 6.29 |
| CHEMBL5436810 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL5398072 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL5436629 | — | IC50 | = | 594.0 | nM | 6.23 |
| CHEMBL5435681 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5422753 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5410611 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL5407884 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL5413084 | — | IC50 | = | 932.0 | nM | 6.03 |
| CHEMBL5427214 | — | IC50 | = | 976.0 | nM | 6.01 |
| CHEMBL5408544 | — | IC50 | = | 2768.0 | nM | 5.56 |
| CHEMBL5400037 | — | IC50 | = | 2758.0 | nM | 5.56 |
| CHEMBL5414869 | — | IC50 | = | 3487.0 | nM | 5.46 |
| CHEMBL5401441 | — | IC50 | = | 4494.0 | nM | 5.35 |
| CHEMBL5435016 | — | IC50 | = | 6133.0 | nM | 5.21 |
| CHEMBL5426190 | — | IC50 | = | 6319.0 | nM | 5.20 |
| CHEMBL5397019 | — | IC50 | = | 6506.0 | nM | 5.19 |
| CHEMBL5408062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5400253 | — | IC50 | > | 10000.0 | nM | - |