Assay Detail
Binding
CHEMBL4032333
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Inhibition of wild type IDH1 (unknown origin) using isocitrate as substrate preincubated for 30 mins followed by substrate addition in presence of NADP+ measured up to 5 mins by resorufin-based fluorescence assay
21
Total Activities
21
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 Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.43 | 4.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082867 | — | — | 1 | 4.58 |
| CHEMBL4081890 | — | — | 1 | 4.53 |
| CHEMBL4100845 | — | — | 1 | 4.47 |
| CHEMBL4101800 | — | — | 1 | 4.47 |
| CHEMBL4059985 | — | — | 1 | 4.32 |
| CHEMBL4063125 | — | — | 1 | 4.32 |
| CHEMBL4080497 | — | — | 1 | 4.32 |
| CHEMBL3335794 | — | — | 1 | - |
| CHEMBL4065858 | — | — | 1 | - |
| CHEMBL4076973 | — | — | 1 | - |
| CHEMBL4084774 | — | — | 1 | - |
| CHEMBL4099443 | — | — | 1 | - |
| CHEMBL4069796 | — | — | 1 | - |
| CHEMBL4090794 | — | — | 1 | - |
| CHEMBL2059811 | — | — | 1 | - |
| CHEMBL4076958 | — | — | 1 | - |
| CHEMBL4066429 | — | — | 1 | - |
| CHEMBL4092360 | — | — | 1 | - |
| CHEMBL4075666 | — | — | 1 | - |
| CHEMBL4090677 | — | — | 1 | - |
| CHEMBL4076027 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082867 | — | IC50 | = | 26600.0 | nM | 4.58 |
| CHEMBL4081890 | — | IC50 | = | 29800.0 | nM | 4.53 |
| CHEMBL4100845 | — | IC50 | = | 33500.0 | nM | 4.47 |
| CHEMBL4101800 | — | IC50 | = | 33500.0 | nM | 4.47 |
| CHEMBL4059985 | — | IC50 | = | 47400.0 | nM | 4.32 |
| CHEMBL4063125 | — | IC50 | = | 47400.0 | nM | 4.32 |
| CHEMBL4080497 | — | IC50 | = | 47400.0 | nM | 4.32 |
| CHEMBL3335794 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4065858 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4076973 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4084774 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4099443 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4069796 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4090794 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL2059811 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4076958 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4066429 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4092360 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4075666 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4090677 | — | IC50 | > | 57000.0 | nM | - |
| CHEMBL4076027 | — | IC50 | > | 57000.0 | nM | - |