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Assay Detail

CHEMBL1917973

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

Binding
Inhibition of recombinant human 5-LOX in human PBML assessed as inhibition of A23187-induced LTB4 production preincubated for 15 mins measured after 15 mins by enzyme immunoassay
15
Total Activities
15
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

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of benzo[1.3.2]dithiazolium ylide 1,1-dioxide derivatives as potential dual cyclooxygenase-2/5-lipoxygenase inhibitors.
Tan CM, Chen GS, Chen CS, Chang PT, Chern JW.
Bioorg Med Chem (2011) 19 : 6316 -6328
PubMed 21958737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.82 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 7.60
CHEMBL1917102 1 6.82
CHEMBL1917097 1 6.75
CHEMBL1917099 1 6.52
CHEMBL1917100 1 6.46
CHEMBL1917098 1 6.44
CHEMBL1917101 1 6.17
CHEMBL1917103 1 5.51
CHEMBL1917086 1 5.46
CHEMBL1917105 1 5.43
CHEMBL1917092 1 5.39
CHEMBL1917090 1 5.22
CHEMBL1917088 1 4.87
CHEMBL1917087 1 4.59
CHEMBL1917107 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 25.0 nM 7.60
CHEMBL1917102 IC50 = 150.0 nM 6.82
CHEMBL1917097 IC50 = 180.0 nM 6.75
CHEMBL1917099 IC50 = 300.0 nM 6.52
CHEMBL1917100 IC50 = 350.0 nM 6.46
CHEMBL1917098 IC50 = 360.0 nM 6.44
CHEMBL1917101 IC50 = 680.0 nM 6.17
CHEMBL1917103 IC50 = 3090.0 nM 5.51
CHEMBL1917086 IC50 = 3450.0 nM 5.46
CHEMBL1917105 IC50 = 3700.0 nM 5.43
CHEMBL1917092 IC50 = 4100.0 nM 5.39
CHEMBL1917090 IC50 = 6050.0 nM 5.22
CHEMBL1917088 IC50 = 13500.0 nM 4.87
CHEMBL1917087 IC50 = 25800.0 nM 4.59
CHEMBL1917107 IC50 = 91100.0 nM 4.04