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Assay Detail

CHEMBL4403237

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

Binding
Inhibition of recombinant C-terminal His-tagged human LOXL3 (1 to 753 residues) expressed in CHO cells 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 Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysyl oxidase homolog 3 (CHEMBL4105989)
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.46 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1618272 1 6.51
CHEMBL4568508 1 6.07
CHEMBL4457897 1 5.91
CHEMBL4444163 1 5.90
CHEMBL4441069 1 5.42
CHEMBL4550042 1 5.41
CHEMBL4564074 1 5.17
CHEMBL4574361 1 5.17
CHEMBL4551909 1 5.03
CHEMBL4441173 1 4.87
CHEMBL4463882 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1618272 IC50 = 310.0 nM 6.51
CHEMBL4568508 IC50 = 860.0 nM 6.07
CHEMBL4457897 IC50 = 1220.0 nM 5.91
CHEMBL4444163 IC50 = 1250.0 nM 5.90
CHEMBL4441069 IC50 = 3850.0 nM 5.42
CHEMBL4550042 IC50 = 3860.0 nM 5.41
CHEMBL4564074 IC50 = 6780.0 nM 5.17
CHEMBL4574361 IC50 = 6690.0 nM 5.17
CHEMBL4551909 IC50 = 9310.0 nM 5.03
CHEMBL4441173 IC50 = 13490.0 nM 4.87
CHEMBL4463882 IC50 = 24240.0 nM 4.62