Assay Detail
Binding
CHEMBL4812388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDH1 R132H mutant (unknown origin) assessed as reduction in NADPH consumption using alpha-KG as substrate incubated for 5 mins by diaphorase/resazurin-coupled system
95
Total Activities
91
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 and Optimization of 2<i>H</i>-1λ<sup>2</sup>-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 95 | 6.29 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4875277 | — | — | 1 | 7.46 |
| CHEMBL4851708 | — | — | 1 | 7.41 |
| CHEMBL4864243 | — | — | 1 | 7.36 |
| CHEMBL4860083 | — | — | 1 | 7.36 |
| CHEMBL4878489 | — | — | 1 | 7.36 |
| CHEMBL4868649 | — | — | 1 | 7.36 |
| CHEMBL4858156 | — | — | 1 | 7.31 |
| CHEMBL4879014 | — | — | 1 | 7.26 |
| CHEMBL4848154 | — | — | 1 | 7.26 |
| CHEMBL4878829 | — | — | 1 | 7.25 |
| CHEMBL4854924 | — | — | 1 | 7.21 |
| CHEMBL3989958 | IVOSIDENIB | 4.0 | 1 | 7.19 |
| CHEMBL4864581 | — | — | 1 | 7.12 |
| CHEMBL4867078 | — | — | 1 | 7.12 |
| CHEMBL4845768 | — | — | 1 | 7.11 |
| CHEMBL4448475 | — | — | 3 | 7.09 |
| CHEMBL4873139 | — | — | 1 | 7.03 |
| CHEMBL4861426 | — | — | 1 | 7.03 |
| CHEMBL4853810 | — | — | 1 | 7.00 |
| CHEMBL4864789 | — | — | 1 | 6.96 |
| CHEMBL4851468 | — | — | 3 | 6.94 |
| CHEMBL4863979 | — | — | 1 | 6.89 |
| CHEMBL4876847 | — | — | 1 | 6.85 |
| CHEMBL4872718 | — | — | 1 | 6.80 |
| CHEMBL4857251 | — | — | 1 | 6.80 |
| CHEMBL4857311 | — | — | 1 | 6.68 |
| CHEMBL4852045 | — | — | 1 | 6.62 |
| CHEMBL4872262 | — | — | 1 | 6.62 |
| CHEMBL4877508 | — | — | 1 | 6.58 |
| CHEMBL4866276 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4875277 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4851708 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4868649 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4878489 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4860083 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4864243 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4858156 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4879014 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4848154 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4878829 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4854924 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3989958 | IVOSIDENIB | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4867078 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4864581 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4845768 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4448475 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4861426 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4873139 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4853810 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4864789 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4448475 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4851468 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4851468 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4863979 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4876847 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4857251 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4872718 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4857311 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4872262 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4852045 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4448475 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4877508 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4863768 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4866276 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4854817 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4853662 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4873401 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4851781 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4861915 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4853124 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4851468 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4871710 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4872838 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4866561 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4849269 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4858758 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4868658 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4852318 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4862440 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4847291 | — | IC50 | = | 1100.0 | nM | 5.96 |