Assay Detail
Binding
CHEMBL3390549
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Inhibition of human recombinant alpha1,3-fucosyltransferase 9 using GDP-[14C]-fucose preincubated for 30 mins by liquid scintillation counting
24
Total Activities
13
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
4-galactosyl-N-acetylglucosaminide 3-alpha-L-fucosyltransferase 9 (CHEMBL4985) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and analysis of potential α1,3-fucosyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 10 | - | - |
| Ki | 7 | 4.17 | 4.30 |
| IC50 | 7 | 4.19 | 4.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1232205 | — | — | 3 | 4.31 |
| CHEMBL384759 | — | — | 3 | 4.23 |
| CHEMBL1233147 | GUANOSINE TRIPHOSPHATE | — | 3 | 4.09 |
| CHEMBL3343359 | — | — | 2 | - |
| CHEMBL3343358 | — | — | 2 | - |
| CHEMBL3343357 | — | — | 2 | - |
| CHEMBL3343356 | — | — | 3 | - |
| CHEMBL14830 | ADENOSINE DIPHOSPHATE | 0.5 | 1 | - |
| CHEMBL3343362 | — | — | 1 | - |
| CHEMBL283807 | — | — | 1 | - |
| CHEMBL3343361 | — | — | 1 | - |
| CHEMBL1233551 | — | — | 1 | - |
| CHEMBL3343360 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1232205 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL1232205 | — | Ki | = | 50300.0 | nM | 4.30 |
| CHEMBL384759 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL384759 | — | Ki | = | 77900.0 | nM | 4.11 |
| CHEMBL1233147 | GUANOSINE TRIPHOSPHATE | Ki | = | 80700.0 | nM | 4.09 |
| CHEMBL1233147 | GUANOSINE TRIPHOSPHATE | IC50 | = | 94000.0 | nM | 4.03 |
| CHEMBL3343358 | — | Ki | = | 190000.0 | nM | - |
| CHEMBL3343357 | — | Ki | = | 137000.0 | nM | - |
| CHEMBL3343356 | — | Ki | = | 102000.0 | nM | - |
| CHEMBL3343356 | — | IC50 | = | 104000.0 | nM | - |
| CHEMBL14830 | ADENOSINE DIPHOSPHATE | Inhibition | - | % | - | |
| CHEMBL3343359 | — | Ki | = | 186000.0 | nM | - |
| CHEMBL283807 | — | Inhibition | - | % | - | |
| CHEMBL3343361 | — | Inhibition | - | % | - | |
| CHEMBL1233551 | — | Inhibition | = | 30.0 | % | - |
| CHEMBL3343360 | — | Inhibition | = | 45.0 | % | - |
| CHEMBL3343359 | — | IC50 | = | 247000.0 | nM | - |
| CHEMBL3343358 | — | IC50 | = | 134000.0 | nM | - |
| CHEMBL3343357 | — | IC50 | = | 139000.0 | nM | - |
| CHEMBL3343356 | — | Inhibition | = | 78.0 | % | - |
| CHEMBL1232205 | — | Inhibition | <= | 80.0 | % | - |
| CHEMBL1233147 | GUANOSINE TRIPHOSPHATE | Inhibition | <= | 75.0 | % | - |
| CHEMBL384759 | — | Inhibition | <= | 75.0 | % | - |
| CHEMBL3343362 | — | Inhibition | - | % | - |