Assay Detail
Binding
CHEMBL4326293
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Inhibition of C-terminal 8-His tagged wild type human IDH1 (1 to 414 residues) expressed in Escherichia coli BL21(DE3)-T1R preincubated for 15 mins using isocitrate as substrate in presence of NADP by diaphorase/resazurin coupled fluorescence assay
13
Total Activities
13
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
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.43 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593992 | — | — | 1 | 7.39 |
| CHEMBL4556998 | — | — | 1 | 7.09 |
| CHEMBL4535154 | — | — | 1 | 6.96 |
| CHEMBL4515358 | — | — | 1 | 6.92 |
| CHEMBL4540440 | — | — | 1 | 6.68 |
| CHEMBL221360 | — | — | 1 | 6.57 |
| CHEMBL4548727 | — | — | 1 | 6.39 |
| CHEMBL4215717 | — | — | 1 | 6.01 |
| CHEMBL4549554 | — | — | 1 | 5.82 |
| CHEMBL4551778 | — | — | 1 | 5.75 |
| CHEMBL4459125 | — | — | 1 | 5.10 |
| CHEMBL4562890 | — | — | 1 | - |
| CHEMBL4467995 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593992 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4556998 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4535154 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4515358 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4540440 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL221360 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4548727 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4215717 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4549554 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4551778 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL4459125 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4562890 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4467995 | — | IC50 | > | 10000.0 | nM | - |