Assay Detail
Binding
CHEMBL4332269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-fused IDH1 R132H mutant expressed in Escherichia coli using alpha-ketoglutarate as substrate preincubated for 15 mins followed by substrate addition
30
Total Activities
30
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
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.06 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180727 | — | — | 1 | 7.70 |
| CHEMBL4559482 | — | — | 1 | 7.30 |
| CHEMBL4476190 | — | — | 1 | 7.22 |
| CHEMBL4556914 | — | — | 1 | 7.22 |
| CHEMBL4465287 | — | — | 1 | 7.05 |
| CHEMBL4469450 | — | — | 1 | 7.00 |
| CHEMBL4514241 | — | — | 1 | 6.85 |
| CHEMBL4467855 | — | — | 1 | 6.72 |
| CHEMBL4544382 | — | — | 1 | 6.64 |
| CHEMBL4457293 | — | — | 1 | 6.54 |
| CHEMBL4471506 | — | — | 1 | 6.09 |
| CHEMBL4524313 | — | — | 1 | 6.03 |
| CHEMBL4568252 | — | — | 1 | 6.03 |
| CHEMBL4557985 | — | — | 1 | 6.02 |
| CHEMBL550052 | — | — | 1 | 5.89 |
| CHEMBL4454383 | — | — | 1 | 5.85 |
| CHEMBL4463255 | — | — | 1 | 5.84 |
| CHEMBL4473155 | — | — | 1 | 5.83 |
| CHEMBL4548634 | — | — | 1 | 5.81 |
| CHEMBL4560109 | — | — | 1 | 5.80 |
| CHEMBL4442650 | — | — | 1 | 5.70 |
| CHEMBL4459022 | — | — | 1 | 5.65 |
| CHEMBL4471075 | — | — | 1 | 5.52 |
| CHEMBL4534551 | — | — | 1 | 5.43 |
| CHEMBL4446593 | — | — | 1 | 5.36 |
| CHEMBL4452734 | — | — | 1 | 5.30 |
| CHEMBL4467139 | — | — | 1 | 5.10 |
| CHEMBL4453488 | — | — | 1 | 4.93 |
| CHEMBL4466687 | — | — | 1 | 4.87 |
| CHEMBL4576887 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180727 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4559482 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4476190 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4556914 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4465287 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4469450 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4514241 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4467855 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4544382 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4457293 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4471506 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4524313 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4568252 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4557985 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL550052 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL4454383 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4463255 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL4473155 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4548634 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL4560109 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL4442650 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4459022 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL4471075 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL4534551 | — | IC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL4446593 | — | IC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL4452734 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4467139 | — | IC50 | = | 7910.0 | nM | 5.10 |
| CHEMBL4453488 | — | IC50 | = | 11860.0 | nM | 4.93 |
| CHEMBL4466687 | — | IC50 | = | 13620.0 | nM | 4.87 |
| CHEMBL4576887 | — | IC50 | = | 39600.0 | nM | 4.40 |