Assay Detail
Binding
CHEMBL3860933
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of synthetic recombinant wild type GCase enzyme velaglucerase alfa (unknown origin) at pH 5.9 preincubated for 5 mins followed by addition of 4-Methylumbelliferyl beta-D-glucopyranoside as substrate measured after 30 mins by fluorescence analysis
42
Total Activities
42
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Potent Quinazolines as Selective β-Glucocerebrosidase Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.66 | 8.28 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3976182 | — | — | 1 | 8.28 |
| CHEMBL3939100 | — | — | 1 | 8.19 |
| CHEMBL3930102 | — | — | 1 | 8.09 |
| CHEMBL3923120 | — | — | 1 | 8.08 |
| CHEMBL3950881 | — | — | 1 | 8.06 |
| CHEMBL3923147 | — | — | 1 | 8.00 |
| CHEMBL3976949 | — | — | 1 | 7.90 |
| CHEMBL3956777 | — | — | 1 | 7.70 |
| CHEMBL3956552 | — | — | 1 | 7.68 |
| CHEMBL3964444 | — | — | 1 | 7.57 |
| CHEMBL3968646 | — | — | 1 | 7.53 |
| CHEMBL3941104 | — | — | 1 | 7.46 |
| CHEMBL3974789 | — | — | 1 | 7.38 |
| CHEMBL3948124 | — | — | 1 | 7.25 |
| CHEMBL1193417 | — | — | 1 | 7.01 |
| CHEMBL3906252 | — | — | 1 | 6.91 |
| CHEMBL3929224 | — | — | 1 | 6.90 |
| CHEMBL3957610 | — | — | 1 | 6.78 |
| CHEMBL3920301 | — | — | 1 | 6.75 |
| CHEMBL3980248 | — | — | 1 | 6.63 |
| CHEMBL3965871 | — | — | 1 | 6.60 |
| CHEMBL3970989 | — | — | 1 | 6.55 |
| CHEMBL3963682 | — | — | 1 | 6.39 |
| CHEMBL3894465 | — | — | 1 | 6.37 |
| CHEMBL3968279 | — | — | 1 | 6.14 |
| CHEMBL3970658 | — | — | 1 | 6.09 |
| CHEMBL3898722 | — | — | 1 | 6.07 |
| CHEMBL3932095 | — | — | 1 | 6.06 |
| CHEMBL3921895 | — | — | 1 | 6.05 |
| CHEMBL3908863 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3976182 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3939100 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3930102 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3923120 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3950881 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3923147 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3976949 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL3956777 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3956552 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL3964444 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3968646 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL3941104 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3974789 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3948124 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1193417 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3906252 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3929224 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3957610 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL3920301 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL3980248 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL3965871 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL3970989 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3963682 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL3894465 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL3968279 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3970658 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL3898722 | — | IC50 | = | 857.0 | nM | 6.07 |
| CHEMBL3932095 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL3921895 | — | IC50 | = | 891.0 | nM | 6.05 |
| CHEMBL3908863 | — | IC50 | = | 926.0 | nM | 6.03 |
| CHEMBL3972062 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL3913022 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3942452 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL3944808 | — | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL3914158 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL119841 | — | IC50 | = | 5770.0 | nM | 5.24 |
| CHEMBL3979185 | — | IC50 | = | 28070.0 | nM | 4.55 |
| CHEMBL3912910 | — | IC50 | = | 33210.0 | nM | 4.48 |
| CHEMBL1405704 | — | IC50 | = | 36070.0 | nM | 4.44 |
| CHEMBL3902851 | — | Inhibition | - | % | - | |
| CHEMBL3893897 | — | Inhibition | - | % | - | |
| CHEMBL1591893 | — | Inhibition | - | % | - |