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Assay Detail

CHEMBL619256

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

Binding
Inhibitory activity against 5-lipoxygenase (inhibition of 5-HETE and LTB4 biosynthesis) in bovine polymorphonuclear leukocytes (PMNL).
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Arachidonate 5-lipoxygenase (CHEMBL2980)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Antipsoriatic anthrones with modulated redox properties. 1. Novel 10-substituted 1,8-dihydroxy-9(10H)-anthracenones as inhibitors of 5-lipoxygenase.
Müller K, Gürster D, Piwek S, Wiegrebe W.
J Med Chem (1993) 36 : 4099 -4107
PubMed 8258834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.57 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335405 1 6.52
CHEMBL133113 1 6.52
CHEMBL133805 1 6.40
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 6.40
CHEMBL107703 1 6.30
CHEMBL36648 LONAPALENE 2.0 1 6.30
CHEMBL130560 1 6.30
CHEMBL130302 1 6.30
CHEMBL130038 1 6.22
CHEMBL134029 1 6.00
CHEMBL132621 1 6.00
CHEMBL337845 1 5.70
CHEMBL132745 1 5.70
CHEMBL334954 1 5.70
CHEMBL433846 1 5.52
CHEMBL131667 1 5.40
CHEMBL130581 1 5.22
CHEMBL130382 1 5.22
CHEMBL134069 1 5.16
CHEMBL130209 1 5.00
CHEMBL334941 1 4.96
CHEMBL132990 1 4.96
CHEMBL130360 1 4.85
CHEMBL133058 1 4.85
CHEMBL130792 1 4.77
CHEMBL336428 1 4.77
CHEMBL130968 BUTANTRONE 2.0 1 4.48
CHEMBL46469 ANTHRALIN 2.0 1 4.43
CHEMBL337831 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335405 IC50 = 300.0 nM 6.52
CHEMBL133113 IC50 = 300.0 nM 6.52
CHEMBL133805 IC50 = 400.0 nM 6.40
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 400.0 nM 6.40
CHEMBL107703 IC50 = 500.0 nM 6.30
CHEMBL36648 LONAPALENE IC50 = 500.0 nM 6.30
CHEMBL130560 IC50 = 500.0 nM 6.30
CHEMBL130302 IC50 = 500.0 nM 6.30
CHEMBL130038 IC50 = 600.0 nM 6.22
CHEMBL134029 IC50 = 1000.0 nM 6.00
CHEMBL132621 IC50 = 1000.0 nM 6.00
CHEMBL337845 IC50 = 2000.0 nM 5.70
CHEMBL132745 IC50 = 2000.0 nM 5.70
CHEMBL334954 IC50 = 2000.0 nM 5.70
CHEMBL433846 IC50 = 3000.0 nM 5.52
CHEMBL131667 IC50 = 4000.0 nM 5.40
CHEMBL130581 IC50 = 6000.0 nM 5.22
CHEMBL130382 IC50 = 6000.0 nM 5.22
CHEMBL134069 IC50 = 7000.0 nM 5.16
CHEMBL130209 IC50 = 10000.0 nM 5.00
CHEMBL334941 IC50 = 11000.0 nM 4.96
CHEMBL132990 IC50 = 11000.0 nM 4.96
CHEMBL130360 IC50 = 14000.0 nM 4.85
CHEMBL133058 IC50 = 14000.0 nM 4.85
CHEMBL130792 IC50 = 17000.0 nM 4.77
CHEMBL336428 IC50 = 17000.0 nM 4.77
CHEMBL130968 BUTANTRONE IC50 = 33000.0 nM 4.48
CHEMBL46469 ANTHRALIN IC50 = 37000.0 nM 4.43
CHEMBL337831 IC50 = - nM -