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Assay Detail

CHEMBL2399754

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant DAAO expressed in HEK293 cell lysate assessed as D-Serine conversion to H2O2 after 20 mins by spectrophotometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D-amino-acid oxidase (CHEMBL5485)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase.
Raje M, Hin N, Duvall B, Ferraris DV, Berry JF, Thomas AG, Alt J, Rojas C, Slusher BS, Tsukamoto T.
Bioorg Med Chem Lett (2013) 23 : 3910 -3913
PubMed 23683589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.98 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2397821 1 7.00
CHEMBL2397748 1 6.70
CHEMBL2158320 1 6.70
CHEMBL2158321 1 6.52
CHEMBL2397822 1 6.30
CHEMBL2397742 1 6.30
CHEMBL2397741 1 6.16
CHEMBL2397740 1 6.10
CHEMBL2397745 1 6.10
CHEMBL2397739 1 6.05
CHEMBL2397744 1 6.05
CHEMBL287556 KOJIC ACID 1 5.70
CHEMBL2397743 1 5.52
CHEMBL2158322 1 5.40
CHEMBL2397746 1 4.70
CHEMBL121295 1 4.30
CHEMBL2397823 1 -
CHEMBL2397747 1 -
CHEMBL120412 1 -
CHEMBL448625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2397821 IC50 = 100.0 nM 7.00
CHEMBL2397748 IC50 = 200.0 nM 6.70
CHEMBL2158320 IC50 = 200.0 nM 6.70
CHEMBL2158321 IC50 = 300.0 nM 6.52
CHEMBL2397822 IC50 = 500.0 nM 6.30
CHEMBL2397742 IC50 = 500.0 nM 6.30
CHEMBL2397741 IC50 = 700.0 nM 6.16
CHEMBL2397740 IC50 = 800.0 nM 6.10
CHEMBL2397745 IC50 = 800.0 nM 6.10
CHEMBL2397739 IC50 = 900.0 nM 6.05
CHEMBL2397744 IC50 = 900.0 nM 6.05
CHEMBL287556 KOJIC ACID IC50 = 2000.0 nM 5.70
CHEMBL2397743 IC50 = 3000.0 nM 5.52
CHEMBL2158322 IC50 = 4000.0 nM 5.40
CHEMBL2397746 IC50 = 20000.0 nM 4.70
CHEMBL121295 IC50 = 50000.0 nM 4.30
CHEMBL2397823 IC50 > 100000.0 nM -
CHEMBL2397747 IC50 > 100000.0 nM -
CHEMBL120412 IC50 > 100000.0 nM -
CHEMBL448625 IC50 > 100000.0 nM -