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Assay Detail

CHEMBL1247376

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

Binding
Inhibition of human recombinant VAP-1 expressed in CHO cells after 30 mins by coupled colorimetric method
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Amine oxidase [copper-containing] 3 (CHEMBL3437)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1.
Nurminen EM, Pihlavisto M, Lázár L, Szakonyi Z, Pentikäinen U, Fülöp F, Pentikäinen OT.
J Med Chem (2010) 53 : 6301 -6315
PubMed 20690686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.64 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089 PHENELZINE 4.0 1 7.70
CHEMBL1241119 1 7.54
CHEMBL1241071 1 7.28
CHEMBL1241428 1 7.23
CHEMBL1240954 1 7.22
CHEMBL1241070 1 7.19
CHEMBL1240910 1 7.15
CHEMBL1241004 1 7.10
CHEMBL1240912 1 7.05
CHEMBL1240878 1 7.04
CHEMBL1240877 1 6.96
CHEMBL1240879 1 6.96
CHEMBL1240909 1 6.92
CHEMBL1240908 1 6.77
CHEMBL1241003 1 6.74
CHEMBL1241167 1 6.70
CHEMBL1241120 1 6.68
CHEMBL1241166 1 6.66
CHEMBL1241378 1 6.64
CHEMBL1241069 1 6.62
CHEMBL1241068 1 6.59
CHEMBL1241289 1 6.59
CHEMBL1241263 1 6.59
CHEMBL1241379 1 6.57
CHEMBL1241121 1 6.57
CHEMBL1241123 1 6.55
CHEMBL1241122 1 6.51
CHEMBL1241164 1 6.51
CHEMBL1241165 1 6.49
CHEMBL1241330 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089 PHENELZINE IC50 = 19.95 nM 7.70
CHEMBL1241119 IC50 = 28.84 nM 7.54
CHEMBL1241071 IC50 = 52.48 nM 7.28
CHEMBL1241428 IC50 = 58.88 nM 7.23
CHEMBL1240954 IC50 = 60.26 nM 7.22
CHEMBL1241070 IC50 = 64.57 nM 7.19
CHEMBL1240910 IC50 = 70.79 nM 7.15
CHEMBL1241004 IC50 = 79.43 nM 7.10
CHEMBL1240912 IC50 = 89.13 nM 7.05
CHEMBL1240878 IC50 = 91.2 nM 7.04
CHEMBL1240877 IC50 = 109.65 nM 6.96
CHEMBL1240879 IC50 = 109.65 nM 6.96
CHEMBL1240909 IC50 = 120.23 nM 6.92
CHEMBL1240908 IC50 = 169.82 nM 6.77
CHEMBL1241003 IC50 = 181.97 nM 6.74
CHEMBL1241167 IC50 = 199.53 nM 6.70
CHEMBL1241120 IC50 = 208.93 nM 6.68
CHEMBL1241166 IC50 = 218.78 nM 6.66
CHEMBL1241378 IC50 = 229.09 nM 6.64
CHEMBL1241069 IC50 = 239.88 nM 6.62
CHEMBL1241068 IC50 = 257.04 nM 6.59
CHEMBL1241289 IC50 = 257.04 nM 6.59
CHEMBL1241263 IC50 = 257.04 nM 6.59
CHEMBL1241379 IC50 = 269.15 nM 6.57
CHEMBL1241121 IC50 = 269.15 nM 6.57
CHEMBL1241123 IC50 = 281.84 nM 6.55
CHEMBL1241164 IC50 = 309.03 nM 6.51
CHEMBL1241122 IC50 = 309.03 nM 6.51
CHEMBL1241165 IC50 = 323.59 nM 6.49
CHEMBL1241330 IC50 = 323.59 nM 6.49
CHEMBL1241002 IC50 = 323.59 nM 6.49
CHEMBL1240957 IC50 = 331.13 nM 6.48
CHEMBL1241430 IC50 = 346.74 nM 6.46
CHEMBL1240911 IC50 = 346.74 nM 6.46
CHEMBL1241261 IC50 = 346.74 nM 6.46
CHEMBL1241262 IC50 = 346.74 nM 6.46
CHEMBL1240956 IC50 = 346.74 nM 6.46
CHEMBL1240955 IC50 = 371.54 nM 6.43
CHEMBL1243019 IC50 = 389.05 nM 6.41
CHEMBL1241377 IC50 = 398.11 nM 6.40
CHEMBL1241293 IC50 = 407.38 nM 6.39
CHEMBL1241331 IC50 = 407.38 nM 6.39
CHEMBL1241332 IC50 = 416.87 nM 6.38
CHEMBL1241329 IC50 = 426.58 nM 6.37
CHEMBL1241260 IC50 = 426.58 nM 6.37
CHEMBL1241291 IC50 = 436.52 nM 6.36
CHEMBL1241067 IC50 = 436.52 nM 6.36
CHEMBL1241429 IC50 = 467.74 nM 6.33
CHEMBL1241290 IC50 = 562.34 nM 6.25
CHEMBL1241292 IC50 = 575.44 nM 6.24