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Assay Detail

CHEMBL4138635

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

Binding
Inhibition of human MAOA pre-incubated for 10 mins before p-tyramine substrate addition and measured after 10 mins by amplex red reagent-based microplate fluorescence reader analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Amine oxidase [flavin-containing] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazolobenzothiazine-based carbothioamides as new structural leads for the inhibition of monoamine oxidases: design, synthesis, <i>in vitro</i> bioevaluation and molecular docking studies.
Abid SMA, Aslam S, Zaib S, Bakht SM, Ahmad M, Athar MM, Gardiner JM, Iqbal J.
Medchemcomm (2017) 8 : 452 -464
PubMed 30108763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.60 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161420 1 8.52
CHEMBL8706 CLORGILINE 2.0 1 8.35
CHEMBL4169343 1 8.00
CHEMBL4174892 1 8.00
CHEMBL4163558 1 6.33
CHEMBL4174572 1 6.27
CHEMBL4164511 1 6.01
CHEMBL4159772 1 5.96
CHEMBL4167004 1 5.95
CHEMBL4168112 1 5.85
CHEMBL4159922 1 5.75
CHEMBL4174974 1 5.69
CHEMBL4174656 1 5.63
CHEMBL4172754 1 5.51
CHEMBL4160195 1 5.46
CHEMBL4167833 1 5.43
CHEMBL4170413 1 5.39
CHEMBL4164321 1 5.11
CHEMBL4176042 1 5.09
CHEMBL4168191 1 5.04
CHEMBL4166659 1 5.04
CHEMBL4160257 1 4.97
CHEMBL4171534 1 4.57
CHEMBL4171454 1 4.52
CHEMBL4160919 1 4.51
CHEMBL4159846 1 4.47
CHEMBL4170002 1 4.19
CHEMBL4167764 1 4.18
CHEMBL8663 1 4.17
CHEMBL4162079 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161420 IC50 = 3.0 nM 8.52
CHEMBL8706 CLORGILINE IC50 = 4.5 nM 8.35
CHEMBL4169343 IC50 = 10.0 nM 8.00
CHEMBL4174892 IC50 = 10.0 nM 8.00
CHEMBL4163558 IC50 = 470.0 nM 6.33
CHEMBL4174572 IC50 = 540.0 nM 6.27
CHEMBL4164511 IC50 = 970.0 nM 6.01
CHEMBL4159772 IC50 = 1110.0 nM 5.96
CHEMBL4167004 IC50 = 1130.0 nM 5.95
CHEMBL4168112 IC50 = 1420.0 nM 5.85
CHEMBL4159922 IC50 = 1770.0 nM 5.75
CHEMBL4174974 IC50 = 2060.0 nM 5.69
CHEMBL4174656 IC50 = 2330.0 nM 5.63
CHEMBL4172754 IC50 = 3070.0 nM 5.51
CHEMBL4160195 IC50 = 3490.0 nM 5.46
CHEMBL4167833 IC50 = 3690.0 nM 5.43
CHEMBL4170413 IC50 = 4060.0 nM 5.39
CHEMBL4164321 IC50 = 7730.0 nM 5.11
CHEMBL4176042 IC50 = 8180.0 nM 5.09
CHEMBL4168191 IC50 = 9150.0 nM 5.04
CHEMBL4166659 IC50 = 9020.0 nM 5.04
CHEMBL4160257 IC50 = 10600.0 nM 4.97
CHEMBL4171534 IC50 = 27200.0 nM 4.57
CHEMBL4171454 IC50 = 30200.0 nM 4.52
CHEMBL4160919 IC50 = 31200.0 nM 4.51
CHEMBL4159846 IC50 = 33800.0 nM 4.47
CHEMBL4170002 IC50 = 64800.0 nM 4.19
CHEMBL4167764 IC50 = 65700.0 nM 4.18
CHEMBL8663 IC50 = 67250.0 nM 4.17
CHEMBL4162079 IC50 = 76200.0 nM 4.12