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Assay Detail

CHEMBL2173194

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

Binding
Inhibition of human recombinant 5-lipoxygenase-mediated product formation from arachidonic acid after 5 to 10 mins by HPLC analysis
35
Total Activities
35
Compounds Tested
1
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

Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.
Hieke M, Greiner C, Dittrich M, Reisen F, Schneider G, Schubert-Zsilavecz M, Werz O.
J Med Chem (2011) 54 : 4490 -4507
PubMed 21591611 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.36 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314360 1 6.80
CHEMBL1172016 1 5.66
CHEMBL1170264 1 5.66
CHEMBL1172019 1 5.57
CHEMBL1172003 1 5.55
CHEMBL1171652 1 5.55
CHEMBL1173376 1 5.51
CHEMBL1819479 1 5.36
CHEMBL461883 1 5.33
CHEMBL1171851 1 5.31
CHEMBL1819393 1 5.31
CHEMBL1172222 1 5.30
CHEMBL1171831 1 5.18
CHEMBL1172000 1 5.17
CHEMBL1172002 1 5.17
CHEMBL1173121 1 5.16
CHEMBL1819392 1 5.14
CHEMBL1171834 1 5.05
CHEMBL1173499 1 5.05
CHEMBL1172001 1 5.03
CHEMBL1171832 1 5.03
CHEMBL1819480 1 5.00
CHEMBL1819390 1 -
CHEMBL1819391 1 -
CHEMBL1170852 1 -
CHEMBL1819394 1 -
CHEMBL1819395 1 -
CHEMBL1819396 1 -
CHEMBL2170363 1 -
CHEMBL1819397 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314360 IC50 = 160.0 nM 6.80
CHEMBL1172016 IC50 = 2200.0 nM 5.66
CHEMBL1170264 IC50 = 2200.0 nM 5.66
CHEMBL1172019 IC50 = 2700.0 nM 5.57
CHEMBL1172003 IC50 = 2800.0 nM 5.55
CHEMBL1171652 IC50 = 2800.0 nM 5.55
CHEMBL1173376 IC50 = 3100.0 nM 5.51
CHEMBL1819479 IC50 = 4400.0 nM 5.36
CHEMBL461883 IC50 = 4700.0 nM 5.33
CHEMBL1171851 IC50 = 4900.0 nM 5.31
CHEMBL1819393 IC50 = 4900.0 nM 5.31
CHEMBL1172222 IC50 = 5000.0 nM 5.30
CHEMBL1171831 IC50 = 6600.0 nM 5.18
CHEMBL1172000 IC50 = 6800.0 nM 5.17
CHEMBL1172002 IC50 = 6800.0 nM 5.17
CHEMBL1173121 IC50 = 7000.0 nM 5.16
CHEMBL1819392 IC50 = 7200.0 nM 5.14
CHEMBL1171834 IC50 = 9000.0 nM 5.05
CHEMBL1173499 IC50 = 9000.0 nM 5.05
CHEMBL1172001 IC50 = 9300.0 nM 5.03
CHEMBL1171832 IC50 = 9300.0 nM 5.03
CHEMBL1819480 IC50 = 10000.0 nM 5.00
CHEMBL1817687 IC50 > 10000.0 nM -
CHEMBL518507 IC50 > 10000.0 nM -
CHEMBL1171833 IC50 > 10000.0 nM -
CHEMBL1819478 IC50 > 10000.0 nM -
CHEMBL1819398 IC50 > 10000.0 nM -
CHEMBL1819397 IC50 > 10000.0 nM -
CHEMBL2170363 IC50 > 10000.0 nM -
CHEMBL1819396 IC50 > 10000.0 nM -
CHEMBL1819395 IC50 > 10000.0 nM -
CHEMBL1819394 IC50 > 10000.0 nM -
CHEMBL1170852 IC50 > 10000.0 nM -
CHEMBL1819391 IC50 > 10000.0 nM -
CHEMBL1819390 IC50 > 10000.0 nM -