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Assay Detail

CHEMBL1062055

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

Binding
Inhibition of MAO-A from Wistar rat brain by radioenzymatic assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Amine oxidase [flavin-containing] A (CHEMBL3358)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of a novel class of potent coumarin monoamine oxidase B inhibitors: development and biopharmacological profiling of 7-[(3-chlorobenzyl)oxy]-4-[(methylamino)methyl]-2H-chromen-2-one methanesulfonate (NW-1772) as a highly potent, selective, reversible, and orally active monoamine oxidase B inhibitor.
Pisani L, Muncipinto G, Miscioscia TF, Nicolotti O, Leonetti F, Catto M, Caccia C, Salvati P, Soto-Otero R, Mendez-Alvarez E, Passeleu C, Carotti A.
J Med Chem (2009) 52 : 6685 -6706
PubMed 19810674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 4.96 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL572768 1 6.70
CHEMBL575093 1 6.33
CHEMBL575931 1 6.30
CHEMBL572828 1 5.84
CHEMBL575938 1 5.70
CHEMBL572534 1 5.70
CHEMBL573051 1 5.60
CHEMBL573300 1 5.55
CHEMBL574191 1 5.37
CHEMBL572533 1 5.36
CHEMBL573301 1 5.27
CHEMBL593763 1 5.23
CHEMBL575937 1 5.20
CHEMBL574419 1 5.10
CHEMBL575285 1 4.87
CHEMBL573052 1 4.81
CHEMBL573985 1 4.68
CHEMBL575734 1 4.65
CHEMBL577614 1 4.64
CHEMBL573755 1 4.64
CHEMBL585360 1 4.59
CHEMBL575738 1 4.58
CHEMBL573986 1 4.58
CHEMBL575486 1 4.50
CHEMBL583128 1 4.46
CHEMBL574860 1 4.29
CHEMBL583587 1 4.16
CHEMBL573988 1 4.13
CHEMBL575735 1 4.04
CHEMBL577175 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL572768 IC50 = 200.0 nM 6.70
CHEMBL575093 IC50 = 470.0 nM 6.33
CHEMBL575931 IC50 = 500.0 nM 6.30
CHEMBL572828 IC50 = 1440.0 nM 5.84
CHEMBL575938 IC50 = 2000.0 nM 5.70
CHEMBL572534 IC50 = 2000.0 nM 5.70
CHEMBL573051 IC50 = 2500.0 nM 5.60
CHEMBL573300 IC50 = 2800.0 nM 5.55
CHEMBL574191 IC50 = 4270.0 nM 5.37
CHEMBL572533 IC50 = 4400.0 nM 5.36
CHEMBL573301 IC50 = 5400.0 nM 5.27
CHEMBL593763 IC50 = 5940.0 nM 5.23
CHEMBL575937 IC50 = 6260.0 nM 5.20
CHEMBL574419 IC50 = 8000.0 nM 5.10
CHEMBL575285 IC50 = 13500.0 nM 4.87
CHEMBL573052 IC50 = 15400.0 nM 4.81
CHEMBL573985 IC50 = 21000.0 nM 4.68
CHEMBL575734 IC50 = 22600.0 nM 4.65
CHEMBL577614 IC50 = 22700.0 nM 4.64
CHEMBL573755 IC50 = 23100.0 nM 4.64
CHEMBL585360 IC50 = 25900.0 nM 4.59
CHEMBL575738 IC50 = 26000.0 nM 4.58
CHEMBL573986 IC50 = 26500.0 nM 4.58
CHEMBL575486 IC50 = 31800.0 nM 4.50
CHEMBL583128 IC50 = 35000.0 nM 4.46
CHEMBL574860 IC50 = 50800.0 nM 4.29
CHEMBL583587 IC50 = 70000.0 nM 4.16
CHEMBL573988 IC50 = 74000.0 nM 4.13
CHEMBL575735 IC50 = 91000.0 nM 4.04
CHEMBL577175 IC50 = 99800.0 nM 4.00
CHEMBL584377 IC50 = 100000.0 nM 4.00
CHEMBL574859 IC50 = 100000.0 nM 4.00
CHEMBL575907 IC50 > 100000.0 nM -
CHEMBL575737 IC50 > 100000.0 nM -
CHEMBL575074 IC50 > 100000.0 nM -
CHEMBL575908 IC50 > 100000.0 nM -
CHEMBL573522 IC50 > 100000.0 nM -
CHEMBL577616 IC50 > 100000.0 nM -
CHEMBL575522 IC50 > 100000.0 nM -
CHEMBL584607 IC50 > 100000.0 nM -
CHEMBL575521 IC50 > 100000.0 nM -
CHEMBL574420 IC50 > 100000.0 nM -