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Assay Detail

CHEMBL5738729

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

Binding
Enzyme Activity Assay:: The inhibition of the sample on VAP-1 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). The fluorescence signal value after the background signal was removed was analyzed by Prism software, and the IC50 of the sample against the VAP-1 enzyme was calculated.
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
(2022)

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
CHEMBL5909558 — — 3 9.70
CHEMBL6034455 — — 3 9.70
CHEMBL5774203 — — 3 9.70
CHEMBL6058433 — — 3 9.70
CHEMBL5976788 — — 3 9.52
CHEMBL5759074 — — 3 9.52
CHEMBL5864694 — — 3 9.52
CHEMBL5889367 — — 3 9.52
CHEMBL6056233 — — 3 9.52
CHEMBL5811353 — — 3 9.52
CHEMBL5886360 — — 3 9.52
CHEMBL6013999 — — 3 9.52
CHEMBL5779219 — — 3 9.52
CHEMBL6031782 — — 3 9.52
CHEMBL5761926 — — 3 9.52
CHEMBL5841363 — — 3 9.40
CHEMBL5740442 — — 3 9.40
CHEMBL5849610 — — 3 9.40
CHEMBL5830578 — — 3 9.40
CHEMBL5840164 — — 3 9.40
CHEMBL5750498 — — 3 9.40
CHEMBL5789816 — — 3 9.40
CHEMBL6020248 — — 3 9.40
CHEMBL5937003 — — 3 9.30
CHEMBL5803362 — — 3 9.30
CHEMBL5757706 — — 3 9.30
CHEMBL5955782 — — 3 9.30
CHEMBL5939417 — — 3 9.30
CHEMBL5848750 — — 3 9.30
CHEMBL5863060 — — 3 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5774203 — IC50 = 0.2 nM 9.70
CHEMBL5909558 — IC50 = 0.2 nM 9.70
CHEMBL6058433 — IC50 = 0.2 nM 9.70
CHEMBL6034455 — IC50 = 0.2 nM 9.70
CHEMBL5761926 — IC50 = 0.3 nM 9.52
CHEMBL5811353 — IC50 = 0.3 nM 9.52
CHEMBL5864694 — IC50 = 0.3 nM 9.52
CHEMBL5779219 — IC50 = 0.3 nM 9.52
CHEMBL6056233 — IC50 = 0.3 nM 9.52
CHEMBL6013999 — IC50 = 0.3 nM 9.52
CHEMBL5889367 — IC50 = 0.3 nM 9.52
CHEMBL6031782 — IC50 = 0.3 nM 9.52
CHEMBL5759074 — IC50 = 0.3 nM 9.52
CHEMBL5976788 — IC50 = 0.3 nM 9.52
CHEMBL5886360 — IC50 = 0.3 nM 9.52
CHEMBL5740442 — IC50 = 0.4 nM 9.40
CHEMBL6020248 — IC50 = 0.4 nM 9.40
CHEMBL5849610 — IC50 = 0.4 nM 9.40
CHEMBL5840164 — IC50 = 0.4 nM 9.40
CHEMBL5841363 — IC50 = 0.4 nM 9.40
CHEMBL5750498 — IC50 = 0.4 nM 9.40
CHEMBL5830578 — IC50 = 0.4 nM 9.40
CHEMBL5789816 — IC50 = 0.4 nM 9.40
CHEMBL5757706 — IC50 = 0.5 nM 9.30
CHEMBL5848750 — IC50 = 0.5 nM 9.30
CHEMBL5955782 — IC50 = 0.5 nM 9.30
CHEMBL5803362 — IC50 = 0.5 nM 9.30
CHEMBL5939417 — IC50 = 0.5 nM 9.30
CHEMBL5937003 — IC50 = 0.5 nM 9.30
CHEMBL5966026 — IC50 = 0.6 nM 9.22
CHEMBL5863060 — IC50 = 0.6 nM 9.22
CHEMBL6011965 — IC50 = 0.7 nM 9.15
CHEMBL6025775 — IC50 = 0.7 nM 9.15
CHEMBL5816953 — IC50 = 0.7 nM 9.15
CHEMBL6029983 — IC50 = 0.7 nM 9.15
CHEMBL6062854 — IC50 = 0.7 nM 9.15
CHEMBL5896050 — IC50 = 0.8 nM 9.10
CHEMBL5955131 — IC50 = 0.8 nM 9.10
CHEMBL5956529 — IC50 = 0.8 nM 9.10
CHEMBL5863461 — IC50 = 0.8 nM 9.10
CHEMBL6035107 — IC50 = 0.8 nM 9.10
CHEMBL6029275 — IC50 = 0.8 nM 9.10
CHEMBL5872242 — IC50 = 0.9 nM 9.05
CHEMBL5832594 — IC50 = 0.9 nM 9.05
CHEMBL6036220 — IC50 = 0.9 nM 9.05
CHEMBL5833041 — IC50 = 1.0 nM 9.00
CHEMBL5766741 — IC50 = 1.0 nM 9.00
CHEMBL5890026 — IC50 = 1.0 nM 9.00
CHEMBL5969607 — IC50 = 1.0 nM 9.00
CHEMBL5783046 — IC50 = 1.0 nM 9.00