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Assay Detail

CHEMBL618020

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

Binding
The compound was tested for the concentration (in uM) to inhibit 50% of 5-Lipoxygenase (5-LOX) and is expressed in IC50.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent.
Janusz JM, Young PA, Ridgeway JM, Scherz MW, Enzweiler K, Wu LI, Gan L, Darolia R, Matthews RS, Hennes D, Kellstein DE, Green SA, Tulich JL, Rosario-Jansen T, Magrisso IJ, Wehmeyer KR, Kuhlenbeck DL, Eichhold TH, Dobson RL, Sirko SP, Farmer RW.
J Med Chem (1998) 41 : 1112 -1123
PubMed 9544211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.13 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13878 TEBUFELONE 2.0 1 5.52
CHEMBL275120 1 5.30
CHEMBL13920 1 5.22
CHEMBL14420 1 5.10
CHEMBL13623 1 5.10
CHEMBL13980 1 5.07
CHEMBL13661 1 4.92
CHEMBL276436 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13878 TEBUFELONE IC50 = 3000.0 nM 5.52
CHEMBL275120 IC50 = 5000.0 nM 5.30
CHEMBL13920 IC50 = 6000.0 nM 5.22
CHEMBL14420 IC50 = 8000.0 nM 5.10
CHEMBL13623 IC50 = 8000.0 nM 5.10
CHEMBL13980 IC50 = 8500.0 nM 5.07
CHEMBL13661 IC50 = 12000.0 nM 4.92
CHEMBL276436 IC50 = 15000.0 nM 4.82