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Assay Detail

CHEMBL615242

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

Binding
Inhibitory activity against conversion of [1-14C]arachidonic acid to 12-HPETE and its reduction product 12-HETE by porcine leukocyte type 12-lipoxygenase
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Arachidonate 12-lipoxygenase (CHEMBL2381)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

(Carboxyalkyl)benzyl propargyl ethers as selective inhibitors of leukocyte-type 12-lipoxygenases.
Gorins G, Kuhnert L, Johnson CR, Marnett LJ.
J Med Chem (1996) 39 : 4871 -4878
PubMed 8960545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.29 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL144207 1 7.46
CHEMBL144564 1 7.40
CHEMBL357912 1 7.30
CHEMBL142250 1 7.22
CHEMBL144091 1 7.00
CHEMBL344557 2 6.55
CHEMBL341664 1 6.50
CHEMBL144581 1 6.50
CHEMBL144092 1 5.70
CHEMBL422311 1 5.60
CHEMBL2112001 1 5.30
CHEMBL359008 1 5.30
CHEMBL359394 1 5.22
CHEMBL144674 1 5.00
CHEMBL145094 1 -
CHEMBL147680 1 -
CHEMBL144178 1 -
CHEMBL143392 1 -
CHEMBL145194 1 -
CHEMBL144297 1 -
CHEMBL144428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL144207 IC50 = 35.0 nM 7.46
CHEMBL144564 IC50 = 40.0 nM 7.40
CHEMBL357912 IC50 = 50.0 nM 7.30
CHEMBL142250 IC50 = 60.0 nM 7.22
CHEMBL144091 IC50 = 100.0 nM 7.00
CHEMBL344557 IC50 = 280.0 nM 6.55
CHEMBL341664 IC50 = 320.0 nM 6.50
CHEMBL144581 IC50 = 320.0 nM 6.50
CHEMBL344557 IC50 = 450.0 nM 6.35
CHEMBL144092 IC50 = 2000.0 nM 5.70
CHEMBL422311 IC50 = 2500.0 nM 5.60
CHEMBL2112001 IC50 = 5000.0 nM 5.30
CHEMBL359008 IC50 = 5000.0 nM 5.30
CHEMBL359394 IC50 = 6000.0 nM 5.22
CHEMBL144674 IC50 = 10000.0 nM 5.00
CHEMBL147680 IC50 > 10000.0 nM -
CHEMBL145094 IC50 > 10000.0 nM -
CHEMBL144178 IC50 > 10000.0 nM -
CHEMBL143392 IC50 > 10000.0 nM -
CHEMBL144297 IC50 > 10000.0 nM -
CHEMBL145194 IC50 > 10000.0 nM -
CHEMBL144428 IC50 > 10000.0 nM -