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Assay Detail

CHEMBL2149156

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

Binding
Inhibition of 5-lipoxygenase in human neutrophils assessed as inhibition of LTB4 production
12
Total Activities
12
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

Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.
Baumgartner L, Sosa S, Atanasov AG, Bodensieck A, Fakhrudin N, Bauer J, Favero GD, Ponti C, Heiss EH, Schwaiger S, Ladurner A, Widowitz U, Loggia RD, Rollinger JM, Werz O, Bauer R, Dirsch VM, Tubaro A, Stuppner H.
J Nat Prod (2011) 74 : 1779 -1786
PubMed 21800856 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.72 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93 ZILEUTON 4.0 1 5.20
CHEMBL2147421 1 4.74
CHEMBL2147419 1 4.57
CHEMBL2147415 1 4.38
CHEMBL2147416 1 -
CHEMBL2147417 1 -
CHEMBL2147418 1 -
CHEMBL2147420 1 -
CHEMBL2147422 1 -
CHEMBL2147423 RATANIAPHENOL III 1 -
CHEMBL2147424 RATANIAPHENOL I 1 -
CHEMBL463574 RATANIAPHENOL II 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93 ZILEUTON IC50 = 6300.0 nM 5.20
CHEMBL2147421 IC50 = 18400.0 nM 4.74
CHEMBL2147419 IC50 = 27200.0 nM 4.57
CHEMBL2147415 IC50 = 41400.0 nM 4.38
CHEMBL2147416 IC50 > 50000.0 nM -
CHEMBL2147417 IC50 > 50000.0 nM -
CHEMBL2147418 IC50 > 50000.0 nM -
CHEMBL2147420 IC50 > 50000.0 nM -
CHEMBL2147422 IC50 > 50000.0 nM -
CHEMBL2147423 RATANIAPHENOL III IC50 > 50000.0 nM -
CHEMBL2147424 RATANIAPHENOL I IC50 > 50000.0 nM -
CHEMBL463574 RATANIAPHENOL II IC50 > 50000.0 nM -