Assay Detail
Binding
CHEMBL4138489
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Inhibition of N-terminal His-tagged CSE extracted from human HepG2 cells expressed in Escherichia coli BL21 (DE3) using cysteine as substrate assessed as decrease in H2S production preincubated for 3 mins in presence of lead nitrate followed by cysteine addition
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.40 | 5.40 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL347862 | CARBOXYMETHOXYLAMINE | — | 1 | 5.40 |
| CHEMBL4160717 | — | — | 1 | - |
| CHEMBL164 | MYRICETIN | — | 1 | - |
| CHEMBL65320 | AGATHISFLAVONE | — | 1 | - |
| CHEMBL1208973 | CUPRESSUFLAVONE | — | 1 | - |
| CHEMBL1172216 | SIKOKIANIN C | — | 1 | - |
| CHEMBL220745 | PODOCARPUSFLAVONE A | — | 1 | - |
| CHEMBL4164543 | — | — | 1 | - |
| CHEMBL4167976 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL347862 | CARBOXYMETHOXYLAMINE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4160717 | — | Inhibition | - | % | - | |
| CHEMBL164 | MYRICETIN | Inhibition | - | % | - | |
| CHEMBL65320 | AGATHISFLAVONE | IC50 | > | 400000.0 | nM | - |
| CHEMBL1208973 | CUPRESSUFLAVONE | IC50 | > | 400000.0 | nM | - |
| CHEMBL1172216 | SIKOKIANIN C | IC50 | > | 400000.0 | nM | - |
| CHEMBL220745 | PODOCARPUSFLAVONE A | IC50 | > | 400000.0 | nM | - |
| CHEMBL4164543 | — | IC50 | > | 400000.0 | nM | - |
| CHEMBL4167976 | — | IC50 | > | 400000.0 | nM | - |