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Assay Detail

CHEMBL919562

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

Functional
Inhibition of 5LOX in human whole blood assessed as inhibition of calcium ionophore A 23187-stimulated 5HETE production by HPLC analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

New COX-2/5-LOX inhibitors: apoptosis-inducing agents potentially useful in prostate cancer chemotherapy.
Pommery N, Taverne T, Telliez A, Goossens L, Charlier C, Pommery J, Goossens JF, Houssin R, Durant F, Hénichart JP.
J Med Chem (2004) 47 : 6195 -6206
PubMed 15566290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.26 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20403 ZD-2138 1 7.08
CHEMBL423638 1 6.52
CHEMBL375308 1 6.32
CHEMBL223691 1 6.24
CHEMBL384659 1 6.14
CHEMBL374427 1 6.13
CHEMBL222732 1 6.12
CHEMBL222480 1 6.11
CHEMBL426571 1 6.10
CHEMBL222146 1 6.08
CHEMBL222482 1 6.07
CHEMBL118 CELECOXIB 4.0 1 -
CHEMBL222902 1 -
CHEMBL375309 1 -
CHEMBL375127 1 -
CHEMBL222531 1 -
CHEMBL376711 1 -
CHEMBL373514 1 -
CHEMBL373434 1 -
CHEMBL436494 1 -
CHEMBL225463 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20403 ZD-2138 IC50 = 83.0 nM 7.08
CHEMBL423638 IC50 = 300.0 nM 6.52
CHEMBL375308 IC50 = 480.0 nM 6.32
CHEMBL223691 IC50 = 570.0 nM 6.24
CHEMBL384659 IC50 = 720.0 nM 6.14
CHEMBL374427 IC50 = 740.0 nM 6.13
CHEMBL222732 IC50 = 760.0 nM 6.12
CHEMBL222480 IC50 = 770.0 nM 6.11
CHEMBL426571 IC50 = 800.0 nM 6.10
CHEMBL222146 IC50 = 830.0 nM 6.08
CHEMBL222482 IC50 = 850.0 nM 6.07
CHEMBL118 CELECOXIB IC50 > 10000.0 nM -
CHEMBL222902 IC50 > 10000.0 nM -
CHEMBL375309 IC50 > 10000.0 nM -
CHEMBL375127 IC50 > 10000.0 nM -
CHEMBL222531 IC50 > 10000.0 nM -
CHEMBL376711 IC50 > 10000.0 nM -
CHEMBL373514 IC50 > 10000.0 nM -
CHEMBL373434 IC50 > 10000.0 nM -
CHEMBL436494 IC50 > 10000.0 nM -
CHEMBL225463 IC50 > 10000.0 nM -