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Assay Detail

CHEMBL4403232

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

Binding
Inhibition of human C-terminal His10-tagged LOXL2 (Met1 to Gln774 residues) expressed in mouse NS0 cells using cadaverine hydrochloride as substrate preincubated for 1 hr followed by substrate addition by ROS-Glo assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Lysyl oxidase homolog 2 (CHEMBL3714029)
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 38 6.36 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4568508 1 7.07
CHEMBL4515085 1 6.99
CHEMBL4457897 1 6.96
CHEMBL4460845 1 6.84
CHEMBL4444163 1 6.82
CHEMBL4468424 1 6.76
CHEMBL4441173 1 6.75
CHEMBL4467411 1 6.74
CHEMBL4545533 1 6.72
CHEMBL4441130 1 6.63
CHEMBL4441069 1 6.63
CHEMBL4462499 1 6.59
CHEMBL4442153 1 6.59
CHEMBL4457629 1 6.55
CHEMBL4565733 1 6.55
CHEMBL4550042 1 6.52
CHEMBL4586111 1 6.51
CHEMBL4447452 1 6.47
CHEMBL4470882 1 6.46
CHEMBL4574361 1 6.43
CHEMBL4564074 1 6.42
CHEMBL4540485 1 6.41
CHEMBL4450748 1 6.40
CHEMBL4457668 1 6.37
CHEMBL4463882 1 6.37
CHEMBL4466690 1 6.26
CHEMBL4456211 1 6.22
CHEMBL4551909 1 6.19
CHEMBL1618272 1 6.18
CHEMBL4552697 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4568508 IC50 = 86.0 nM 7.07
CHEMBL4515085 IC50 = 103.0 nM 6.99
CHEMBL4457897 IC50 = 109.0 nM 6.96
CHEMBL4460845 IC50 = 143.0 nM 6.84
CHEMBL4444163 IC50 = 151.0 nM 6.82
CHEMBL4468424 IC50 = 174.0 nM 6.76
CHEMBL4441173 IC50 = 176.0 nM 6.75
CHEMBL4467411 IC50 = 184.0 nM 6.74
CHEMBL4545533 IC50 = 192.0 nM 6.72
CHEMBL4441130 IC50 = 236.0 nM 6.63
CHEMBL4441069 IC50 = 233.0 nM 6.63
CHEMBL4462499 IC50 = 255.0 nM 6.59
CHEMBL4442153 IC50 = 259.0 nM 6.59
CHEMBL4457629 IC50 = 280.0 nM 6.55
CHEMBL4565733 IC50 = 280.0 nM 6.55
CHEMBL4550042 IC50 = 302.0 nM 6.52
CHEMBL4586111 IC50 = 310.0 nM 6.51
CHEMBL4447452 IC50 = 342.0 nM 6.47
CHEMBL4470882 IC50 = 343.0 nM 6.46
CHEMBL4574361 IC50 = 370.0 nM 6.43
CHEMBL4564074 IC50 = 380.0 nM 6.42
CHEMBL4540485 IC50 = 394.0 nM 6.41
CHEMBL4450748 IC50 = 397.0 nM 6.40
CHEMBL4457668 IC50 = 423.0 nM 6.37
CHEMBL4463882 IC50 = 425.0 nM 6.37
CHEMBL4466690 IC50 = 554.0 nM 6.26
CHEMBL4456211 IC50 = 606.0 nM 6.22
CHEMBL4551909 IC50 = 652.0 nM 6.19
CHEMBL1618272 IC50 = 665.0 nM 6.18
CHEMBL4552697 IC50 = 671.0 nM 6.17
CHEMBL4528500 IC50 = 686.0 nM 6.16
CHEMBL4443558 IC50 = 810.0 nM 6.09
CHEMBL4456682 IC50 = 828.0 nM 6.08
CHEMBL4475714 IC50 = 1040.0 nM 5.98
CHEMBL4559508 IC50 = 1596.0 nM 5.80
CHEMBL4463323 IC50 = 2164.0 nM 5.67
CHEMBL4565942 IC50 = 6020.0 nM 5.22
CHEMBL4460658 IC50 = 68260.0 nM 4.17