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Assay Detail

CHEMBL618069

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

Binding
Inhibition of 5-lipoxygenase in rat RBL-1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RBL-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
Hanko R, Hammond MD, Fruchtmann R, Pfitzner J, Place GA.
J Med Chem (1990) 33 : 1163 -1170
PubMed 2319562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.24 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275185 1 5.75
CHEMBL274642 BW-755C 1 5.70
CHEMBL276767 1 5.57
CHEMBL17216 1 5.28
CHEMBL8425 NAFAZATROM 2.0 1 5.22
CHEMBL422751 1 5.21
CHEMBL16979 1 5.14
CHEMBL16962 1 5.13
CHEMBL16893 1 5.05
CHEMBL17243 1 4.95
CHEMBL17067 1 4.66
CHEMBL6 INDOMETHACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275185 IC50 = 1800.0 nM 5.75
CHEMBL274642 BW-755C IC50 = 2000.0 nM 5.70
CHEMBL276767 IC50 = 2700.0 nM 5.57
CHEMBL17216 IC50 = 5200.0 nM 5.28
CHEMBL8425 NAFAZATROM IC50 = 6000.0 nM 5.22
CHEMBL422751 IC50 = 6200.0 nM 5.21
CHEMBL16979 IC50 = 7200.0 nM 5.14
CHEMBL16962 IC50 = 7400.0 nM 5.13
CHEMBL16893 IC50 = 9000.0 nM 5.05
CHEMBL17243 IC50 = 11200.0 nM 4.95
CHEMBL17067 IC50 = 22000.0 nM 4.66
CHEMBL6 INDOMETHACIN IC50 >> 20000.0 nM -