Assay Detail
Binding
CHEMBL4672391
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis
12
Total Activities
12
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
Aspartyl/asparaginyl beta-hydroxylase (CHEMBL4680030) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.71 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316034 | — | — | 1 | 7.70 |
| CHEMBL51483 | GOSSYPOL | 3.0 | 1 | 6.48 |
| CHEMBL443684 | NAVITOCLAX | 3.0 | 1 | 5.92 |
| CHEMBL3137309 | VENETOCLAX | 4.0 | 1 | 5.80 |
| CHEMBL6067492 | BLEOMYCIN | 4.0 | 1 | 5.78 |
| CHEMBL376408 | ABT 737 | 1.0 | 1 | 5.52 |
| CHEMBL257619 | — | — | 1 | 5.47 |
| CHEMBL356769 | TUBACIN | — | 1 | 5.45 |
| CHEMBL408513 | BELINOSTAT | 4.0 | 1 | 5.32 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.22 |
| CHEMBL4777255 | — | — | 1 | 5.03 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316034 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL51483 | GOSSYPOL | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL443684 | NAVITOCLAX | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL3137309 | VENETOCLAX | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL6067492 | BLEOMYCIN | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL376408 | ABT 737 | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL257619 | — | IC50 | = | 3390.0 | nM | 5.47 |
| CHEMBL356769 | TUBACIN | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL408513 | BELINOSTAT | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL608533 | MIDOSTAURIN | IC50 | = | 6020.0 | nM | 5.22 |
| CHEMBL4777255 | — | IC50 | = | 9440.0 | nM | 5.03 |
| CHEMBL1229517 | VEMURAFENIB | IC50 | = | 16900.0 | nM | 4.77 |