Assay Detail
Binding
CHEMBL5733693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Assay: Human DAAO enzyme was supplied by the Takeda Pharmaceutical Company (Osaka) and each batch was tested and used at concentrations giving comparable levels of activity. The Km of D-Serine was measured for each enzyme batch to maintain consistency; this Km was used in subsequent assays.On the day of the assay compounds were serially diluted in DMSO before being diluted 1:20 with assay buffer (20 mM Tris ph 7.4). A 5 μl portion of assay buffer was added to the wells of a 384 clear base black-walled plate (Corning), 5 μl of diluted compound was then added via automated plate to plate transfer using the Bravo liquid handler (Agilent technologies) followed by 5 μl of human DAAO enzyme and then 5 μl D-Serine 50 mM was added to all but the negative control wells (final concentration of 10 mM). Finally 5 μl Amplex red reagent (Invitrogen) was added to all wells as per manufacturer's protocol. The plate was incubated for 60 minutes in the dark at 25° C. and the fluorescence in each well was measured in the Envision plate reader.
204
Total Activities
66
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 |
Publication
Pyridazinone compounds and their use as DAAO inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 68 | 7.66 | 8.43 |
| kon | 68 | - | - |
| k_off | 68 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3930320 | — | — | 3 | 8.43 |
| CHEMBL3905105 | — | — | 3 | 8.22 |
| CHEMBL3974794 | — | — | 3 | 8.08 |
| CHEMBL2338797 | — | — | 3 | 8.01 |
| CHEMBL2338800 | — | — | 3 | 8.00 |
| CHEMBL2338786 | — | — | 3 | 8.00 |
| CHEMBL3978036 | — | — | 3 | 8.00 |
| CHEMBL3921356 | — | — | 3 | 8.00 |
| CHEMBL2338803 | — | — | 3 | 7.96 |
| CHEMBL3937708 | — | — | 3 | 7.92 |
| CHEMBL3948886 | — | — | 3 | 7.92 |
| CHEMBL3890910 | — | — | 3 | 7.92 |
| CHEMBL3907451 | — | — | 3 | 7.92 |
| CHEMBL3965028 | — | — | 3 | 7.89 |
| CHEMBL3986233 | — | — | 3 | 7.89 |
| CHEMBL3969619 | — | — | 3 | 7.89 |
| CHEMBL2338795 | — | — | 3 | 7.89 |
| CHEMBL3925924 | — | — | 3 | 7.89 |
| CHEMBL2338790 | — | — | 3 | 7.89 |
| CHEMBL3959707 | — | — | 3 | 7.89 |
| CHEMBL3982802 | — | — | 3 | 7.85 |
| CHEMBL3966850 | — | — | 3 | 7.85 |
| CHEMBL3929576 | — | — | 3 | 7.85 |
| CHEMBL3893956 | — | — | 3 | 7.82 |
| CHEMBL3967423 | — | — | 3 | 7.82 |
| CHEMBL3946543 | — | — | 3 | 7.82 |
| CHEMBL3931005 | — | — | 3 | 7.82 |
| CHEMBL3968355 | — | — | 3 | 7.80 |
| CHEMBL2338798 | — | — | 3 | 7.80 |
| CHEMBL3897961 | — | — | 3 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3930320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3905105 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3974794 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2338797 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL2338786 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2338800 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3978036 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3921356 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2338803 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3937708 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3890910 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3948886 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3907451 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3959707 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3925924 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3965028 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2338795 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3986233 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3969619 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2338790 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3966850 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3929576 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3982802 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3893956 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3931005 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3946543 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3967423 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2338798 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3897961 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3968355 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3892561 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3983879 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3942533 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2338801 | LUVADAXISTAT | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3942392 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3906530 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3969148 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3932199 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3958088 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3906910 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3898429 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3928039 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3928039 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3958627 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3908129 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3965884 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3951636 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3908129 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3975855 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3896184 | — | IC50 | = | 26.0 | nM | 7.58 |