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Assay Detail

CHEMBL1036479

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

Binding
Inhibition of 5-lipoxygenase in bovine polymorphonuclear leucocytes assessed as formation of LTB4 by HPLC method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).
Liedtke AJ, Keck PR, Lehmann F, Koeberle A, Werz O, Laufer SA.
J Med Chem (2009) 52 : 4968 -4972
PubMed 19719242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.35 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300982 LICOFELONE 2.0 1 6.75
CHEMBL57062 1 6.75
CHEMBL560897 1 6.64
CHEMBL563280 1 6.60
CHEMBL550894 1 6.58
CHEMBL565159 1 6.51
CHEMBL564318 1 6.30
CHEMBL292239 1 5.82
CHEMBL294159 1 5.80
CHEMBL550489 1 5.72
CHEMBL29097 1 -
CHEMBL182032 1 -
CHEMBL549341 1 -
CHEMBL561824 1 -
CHEMBL560898 1 -
CHEMBL551236 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300982 LICOFELONE IC50 = 180.0 nM 6.75
CHEMBL57062 IC50 = 180.0 nM 6.75
CHEMBL560897 IC50 = 230.0 nM 6.64
CHEMBL563280 IC50 = 250.0 nM 6.60
CHEMBL550894 IC50 = 260.0 nM 6.58
CHEMBL565159 IC50 = 310.0 nM 6.51
CHEMBL564318 IC50 = 500.0 nM 6.30
CHEMBL292239 IC50 = 1500.0 nM 5.82
CHEMBL294159 IC50 = 1600.0 nM 5.80
CHEMBL550489 IC50 = 1900.0 nM 5.72
CHEMBL29097 IC50 - -
CHEMBL182032 IC50 - -
CHEMBL549341 IC50 - -
CHEMBL561824 IC50 - -
CHEMBL560898 IC50 - -
CHEMBL551236 IC50 - -