Assay Detail
Binding
CHEMBL3887487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Assay: The functional activity of compounds inhibiting the DAAO enzyme was determined by utilizing the co-product of the catalysis of D-Serine, H2O2 which can be quantitatively measured using the Amplex Red (Invitrogen) detection. Amplex Red reagent is a colorless substrate that reacts with hydrogen peroxide (H2O2) with a 1:1 stoichiometry in the presence of hydrogen peroxide to produce highly fluorescent resorufin (excitation/emission maxima=570/585 nm). The changes in fluorescence were monitored by a fluorescence plate reader, Envision (Perkin Elmer) and increases in DAAO activity were readily detected upon addition of D-Serine and suppression of this response observed with the application of test compounds.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.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
5- or 6-substituted 3-hydroxy-2 (1 H)-pyridinones as D-amino acid oxidase (DAAO) inhibitors in therapy of diseases such as schizophrenia, cognitive disorder and pain
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.67 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3905206 | — | — | 1 | 7.54 |
| CHEMBL3894259 | — | — | 1 | 7.46 |
| CHEMBL3977283 | — | — | 1 | 7.35 |
| CHEMBL3971034 | — | — | 1 | 7.33 |
| CHEMBL3908508 | — | — | 1 | 7.28 |
| CHEMBL3946312 | — | — | 1 | 7.26 |
| CHEMBL3978887 | — | — | 1 | 7.21 |
| CHEMBL3892689 | — | — | 1 | 7.10 |
| CHEMBL3922910 | — | — | 1 | 7.08 |
| CHEMBL3982073 | — | — | 1 | 7.00 |
| CHEMBL3917689 | — | — | 1 | 6.89 |
| CHEMBL3917465 | — | — | 1 | 6.89 |
| CHEMBL3926648 | — | — | 1 | 6.89 |
| CHEMBL2338785 | — | — | 1 | 6.85 |
| CHEMBL3922993 | — | — | 1 | 6.80 |
| CHEMBL3983751 | — | — | 1 | 6.77 |
| CHEMBL3932148 | — | — | 1 | 6.72 |
| CHEMBL3919741 | — | — | 1 | 6.72 |
| CHEMBL3906223 | — | — | 1 | 6.68 |
| CHEMBL3912489 | — | — | 1 | 6.64 |
| CHEMBL3933219 | — | — | 1 | 6.62 |
| CHEMBL3968785 | — | — | 1 | 6.60 |
| CHEMBL3907406 | — | — | 1 | 6.58 |
| CHEMBL3931854 | — | — | 1 | 6.46 |
| CHEMBL3944630 | — | — | 1 | 6.44 |
| CHEMBL3901512 | — | — | 1 | 6.41 |
| CHEMBL3953346 | — | — | 1 | 6.34 |
| CHEMBL3972972 | — | — | 1 | 6.31 |
| CHEMBL3930262 | — | — | 1 | 6.31 |
| CHEMBL3890823 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3905206 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3894259 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3977283 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3971034 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3908508 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3946312 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3978887 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3892689 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3922910 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3982073 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3917689 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3917465 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3926648 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2338785 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3922993 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3983751 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3919741 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3932148 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3906223 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3912489 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3933219 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3968785 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3907406 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3931854 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3944630 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3901512 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3953346 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3972972 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3930262 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3890823 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3964353 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3893079 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3896835 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3967757 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3891413 | — | IC50 | = | 1900.0 | nM | 5.72 |