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Assay Detail

CHEMBL1777435

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

Binding
Inhibition of 5-LO in human polymorphonuclear leukocytes assessed as inhibition of LTB4 production after 10 mins by RP-HPLC assay
19
Total Activities
10
Compounds Tested
2
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

Pharmacophore modeling and virtual screening for novel acidic inhibitors of microsomal prostaglandin E₂ synthase-1 (mPGES-1).
Waltenberger B, Wiechmann K, Bauer J, Markt P, Noha SM, Wolber G, Rollinger JM, Werz O, Schuster D, Stuppner H.
J Med Chem (2011) 54 : 3163 -3174
PubMed 21466167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.64 6.96
Inhibition 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314360 1 6.96
CHEMBL1774309 2 6.07
CHEMBL1378043 2 5.64
CHEMBL1774310 2 5.57
CHEMBL1324382 2 5.55
CHEMBL1774311 2 5.35
CHEMBL1774306 2 5.33
CHEMBL565883 2 5.27
CHEMBL1774307 2 5.01
CHEMBL1774308 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314360 IC50 = 110.0 nM 6.96
CHEMBL1774309 IC50 = 850.0 nM 6.07
CHEMBL1378043 IC50 = 2300.0 nM 5.64
CHEMBL1774310 IC50 = 2700.0 nM 5.57
CHEMBL1324382 IC50 = 2800.0 nM 5.55
CHEMBL1774311 IC50 = 4500.0 nM 5.35
CHEMBL1774306 IC50 = 4700.0 nM 5.33
CHEMBL565883 IC50 = 5400.0 nM 5.27
CHEMBL1774307 IC50 = 9800.0 nM 5.01
CHEMBL1378043 Inhibition - % -
CHEMBL1774311 Inhibition - % -
CHEMBL1774310 Inhibition - % -
CHEMBL1774309 Inhibition - % -
CHEMBL1774308 Inhibition - % -
CHEMBL1774307 Inhibition - % -
CHEMBL1324382 Inhibition - % -
CHEMBL565883 Inhibition - % -
CHEMBL1774306 Inhibition - % -
CHEMBL1774308 IC50 > 10000.0 nM -