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Assay Detail

CHEMBL5736786

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Binding
Enzyme Activity Assay: The inhibition of the sample on VAP-enzyme activity was measured by using an Amplex® Red Monoamine Oxidase kit (Invitrogen #A12214). 100 nL of the gradiently-diluted to-be-tested compound (solvent DMSO) was added to a 384-well plate. 25 μL of 10 nM VAP-1 enzyme solution was added and incubated for 30 minutes at room temperature. A substrate mixture of VAP-1 enzyme (200 μM Amplex Red, 1 U/mL HRP, 1 mM Benzylamine) was added and incubated for 60 minutes at room temperature. After the incubation, the fluorescent signal was read with a microplate reader Envision (excitation light wavelength 530-560 nm, emission light wavelength 590 nm).
ChEMBL ↗
243
Total Activities
81
Compounds Tested
3
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 [copper-containing] 3 (CHEMBL3437) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SSAO inhibitor
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 81 9.09 9.70
kon 81 - -
k_off 81 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6001768 — — 3 9.70
CHEMBL6016570 — — 3 9.70
CHEMBL5884221 — — 3 9.70
CHEMBL5977694 — — 3 9.70
CHEMBL5769606 — — 3 9.52
CHEMBL5879186 — — 3 9.52
CHEMBL6013600 — — 3 9.52
CHEMBL5810939 — — 3 9.52
CHEMBL6010009 — — 3 9.52
CHEMBL6042185 — — 3 9.52
CHEMBL5752011 — — 3 9.52
CHEMBL5801027 — — 3 9.52
CHEMBL6027951 — — 3 9.52
CHEMBL5900558 — — 3 9.52
CHEMBL5993055 — — 3 9.52
CHEMBL5832926 — — 3 9.40
CHEMBL5990582 — — 3 9.40
CHEMBL5815932 — — 3 9.40
CHEMBL5999329 — — 3 9.40
CHEMBL5744052 — — 3 9.40
CHEMBL5828586 — — 3 9.40
CHEMBL6026682 — — 3 9.40
CHEMBL6048376 — — 3 9.40
CHEMBL5757808 — — 3 9.30
CHEMBL5769391 — — 3 9.30
CHEMBL5837107 — — 3 9.30
CHEMBL5774758 — — 3 9.30
CHEMBL5741767 — — 3 9.30
CHEMBL5778384 — — 3 9.30
CHEMBL6020114 — — 3 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5884221 — IC50 = 0.2 nM 9.70
CHEMBL6001768 — IC50 = 0.2 nM 9.70
CHEMBL5977694 — IC50 = 0.2 nM 9.70
CHEMBL6016570 — IC50 = 0.2 nM 9.70
CHEMBL5993055 — IC50 = 0.3 nM 9.52
CHEMBL6042185 — IC50 = 0.3 nM 9.52
CHEMBL6013600 — IC50 = 0.3 nM 9.52
CHEMBL6027951 — IC50 = 0.3 nM 9.52
CHEMBL6010009 — IC50 = 0.3 nM 9.52
CHEMBL5801027 — IC50 = 0.3 nM 9.52
CHEMBL5810939 — IC50 = 0.3 nM 9.52
CHEMBL5900558 — IC50 = 0.3 nM 9.52
CHEMBL5879186 — IC50 = 0.3 nM 9.52
CHEMBL5769606 — IC50 = 0.3 nM 9.52
CHEMBL5752011 — IC50 = 0.3 nM 9.52
CHEMBL5990582 — IC50 = 0.4 nM 9.40
CHEMBL6048376 — IC50 = 0.4 nM 9.40
CHEMBL5815932 — IC50 = 0.4 nM 9.40
CHEMBL5744052 — IC50 = 0.4 nM 9.40
CHEMBL5832926 — IC50 = 0.4 nM 9.40
CHEMBL5828586 — IC50 = 0.4 nM 9.40
CHEMBL5999329 — IC50 = 0.4 nM 9.40
CHEMBL6026682 — IC50 = 0.4 nM 9.40
CHEMBL5837107 — IC50 = 0.5 nM 9.30
CHEMBL5778384 — IC50 = 0.5 nM 9.30
CHEMBL5774758 — IC50 = 0.5 nM 9.30
CHEMBL5769391 — IC50 = 0.5 nM 9.30
CHEMBL5741767 — IC50 = 0.5 nM 9.30
CHEMBL5757808 — IC50 = 0.5 nM 9.30
CHEMBL5928444 — IC50 = 0.6 nM 9.22
CHEMBL6020114 — IC50 = 0.6 nM 9.22
CHEMBL5898686 — IC50 = 0.7 nM 9.15
CHEMBL5886190 — IC50 = 0.7 nM 9.15
CHEMBL5884168 — IC50 = 0.7 nM 9.15
CHEMBL5872564 — IC50 = 0.7 nM 9.15
CHEMBL5980805 — IC50 = 0.7 nM 9.15
CHEMBL5823390 — IC50 = 0.8 nM 9.10
CHEMBL5982003 — IC50 = 0.8 nM 9.10
CHEMBL5954504 — IC50 = 0.8 nM 9.10
CHEMBL6028695 — IC50 = 0.8 nM 9.10
CHEMBL5918472 — IC50 = 0.8 nM 9.10
CHEMBL6015653 — IC50 = 0.8 nM 9.10
CHEMBL5857114 — IC50 = 0.9 nM 9.05
CHEMBL5790154 — IC50 = 0.9 nM 9.05
CHEMBL6005429 — IC50 = 0.9 nM 9.05
CHEMBL5922676 — IC50 = 1.0 nM 9.00
CHEMBL6048993 — IC50 = 1.0 nM 9.00
CHEMBL5841852 — IC50 = 1.0 nM 9.00
CHEMBL5795909 — IC50 = 1.0 nM 9.00
CHEMBL5916601 — IC50 = 1.0 nM 9.00