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Assay Detail

CHEMBL4403236

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

Binding
Inhibition of pig skin-derived LOX using cadaverine hydrochloride as substrate preincubated for 1 hr followed by substrate addition by ROS-Glo assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.
Smithen DA, Leung LMH, Challinor M, Lawrence R, Tang H, Niculescu-Duvaz D, Pearce SP, Mcleary R, Lopes F, Aljarah M, Brown M, Johnson L, Thomson G, Marais R, Springer C.
J Med Chem (2020) 63 : 2308 -2324
PubMed 31430136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.53 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441173 1 6.14
CHEMBL4441069 1 5.95
CHEMBL4568508 1 5.83
CHEMBL4444163 1 5.73
CHEMBL4457897 1 5.58
CHEMBL1618272 1 5.50
CHEMBL4564074 1 5.16
CHEMBL4551909 1 4.33
CHEMBL4550042 1 -
CHEMBL4574361 1 -
CHEMBL4463882 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441173 IC50 = 728.0 nM 6.14
CHEMBL4441069 IC50 = 1130.0 nM 5.95
CHEMBL4568508 IC50 = 1490.0 nM 5.83
CHEMBL4444163 IC50 = 1860.0 nM 5.73
CHEMBL4457897 IC50 = 2650.0 nM 5.58
CHEMBL1618272 IC50 = 3140.0 nM 5.50
CHEMBL4564074 IC50 = 6910.0 nM 5.16
CHEMBL4551909 IC50 = 46490.0 nM 4.33
CHEMBL4550042 IC50 > 100000.0 nM -
CHEMBL4574361 IC50 > 100000.0 nM -
CHEMBL4463882 IC50 > 100000.0 nM -