Assay Detail
Binding
CHEMBL5105641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GOT1 (unknown origin) using aspartic acid and alpha-ketoglutaric acid as substrates assessed as reduction in absorbance of NADH incubated for 20 mins in presence of MDH1 and NADH by HTS assay
6
Total Activities
6
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
Aspartate aminotransferase, cytoplasmic (CHEMBL2189139) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of a non-competitive GOT1 inhibitor, hydralazine hydrochloride, via a coupling reaction-based high-throughput screening assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.43 | 4.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276832 | HYDRALAZINE | 4.0 | 1 | 4.58 |
| CHEMBL5176149 | — | — | 1 | 4.53 |
| CHEMBL5182989 | — | — | 1 | 4.18 |
| CHEMBL35505 | DIHYDRALAZINE | 3.0 | 1 | - |
| CHEMBL246237 | — | — | 1 | - |
| CHEMBL5170155 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276832 | HYDRALAZINE | IC50 | = | 26620.0 | nM | 4.58 |
| CHEMBL5176149 | — | IC50 | = | 29440.0 | nM | 4.53 |
| CHEMBL5182989 | — | IC50 | = | 65390.0 | nM | 4.18 |
| CHEMBL35505 | DIHYDRALAZINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL246237 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5170155 | — | IC50 | > | 100000.0 | nM | - |