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Assay Detail

CHEMBL5055348

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

Binding
Displacement of [18F]-FEH from MAO-A in mouse brain homogenate incubated for 60 mins by imaging analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL3681)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core.
Kroth H, Oden F, Serra AM, Molette J, Mueller A, Berndt M, Capotosti F, Gabellieri E, Schmitt-Willich H, Hickman D, Pfeifer A, Dinkelborg L, Stephens A.
Bioorg Med Chem (2021) 52 : 116528 -116528
PubMed 34839158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.70 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5082735 1 8.11
CHEMBL5084771 1 7.29
CHEMBL5088921 1 -
CHEMBL5077904 1 -
CHEMBL5090407 1 -
CHEMBL5081662 1 -
CHEMBL5092563 1 -
CHEMBL5081957 1 -
CHEMBL5091624 1 -
CHEMBL5080178 1 -
CHEMBL5084917 1 -
CHEMBL5081126 1 -
CHEMBL5094590 1 -
CHEMBL5083649 1 -
CHEMBL5091757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5082735 IC50 = 7.8 nM 8.11
CHEMBL5084771 IC50 = 51.0 nM 7.29
CHEMBL5088921 IC50 > 1000.0 nM -
CHEMBL5077904 IC50 > 1000.0 nM -
CHEMBL5090407 IC50 > 1000.0 nM -
CHEMBL5081662 IC50 > 1000.0 nM -
CHEMBL5092563 IC50 > 1000.0 nM -
CHEMBL5081957 IC50 > 1000.0 nM -
CHEMBL5091624 IC50 > 1000.0 nM -
CHEMBL5080178 IC50 - -
CHEMBL5084917 IC50 - -
CHEMBL5081126 IC50 - -
CHEMBL5094590 IC50 - -
CHEMBL5083649 IC50 - -
CHEMBL5091757 IC50 - -