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Assay Detail

CHEMBL618017

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Binding
Inhibition of Human 5-lipoxygenase
23
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

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

Publication

Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.
Hutchinson JH, Charleson S, Evans JF, Falgueyret JP, Hoogsteen K, Jones TR, Kargman S, Macdonald D, McFarlane CS, Nicholson DW.
J Med Chem (1995) 38 : 4538 -4547
PubMed 7473582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.26 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140915 3 8.00
CHEMBL275634 1 7.66
CHEMBL141645 1 7.64
CHEMBL341562 1 7.58
CHEMBL342680 1 7.52
CHEMBL337576 1 7.52
CHEMBL140204 1 7.40
CHEMBL415530 1 7.28
CHEMBL138551 1 7.26
CHEMBL341948 1 7.22
CHEMBL437444 1 7.22
CHEMBL342684 1 7.22
CHEMBL410493 1 7.21
CHEMBL140157 1 7.16
CHEMBL139891 1 7.00
CHEMBL142032 1 6.89
CHEMBL341785 1 6.77
CHEMBL341696 1 6.76
CHEMBL344636 1 6.44
CHEMBL29097 1 -
CHEMBL16596 QUIFLAPON 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140915 IC50 = 10.0 nM 8.00
CHEMBL140915 IC50 = 18.0 nM 7.75
CHEMBL275634 IC50 = 22.0 nM 7.66
CHEMBL141645 IC50 = 23.0 nM 7.64
CHEMBL341562 IC50 = 26.0 nM 7.58
CHEMBL342680 IC50 = 30.0 nM 7.52
CHEMBL337576 IC50 = 30.0 nM 7.52
CHEMBL140204 IC50 = 40.0 nM 7.40
CHEMBL415530 IC50 = 52.0 nM 7.28
CHEMBL138551 IC50 = 55.0 nM 7.26
CHEMBL341948 IC50 = 60.0 nM 7.22
CHEMBL437444 IC50 = 60.0 nM 7.22
CHEMBL342684 IC50 = 60.0 nM 7.22
CHEMBL410493 IC50 = 62.0 nM 7.21
CHEMBL140157 IC50 = 70.0 nM 7.16
CHEMBL140915 IC50 = 95.0 nM 7.02
CHEMBL139891 IC50 = 100.0 nM 7.00
CHEMBL142032 IC50 = 130.0 nM 6.89
CHEMBL341785 IC50 = 170.0 nM 6.77
CHEMBL341696 IC50 = 175.0 nM 6.76
CHEMBL344636 IC50 = 360.0 nM 6.44
CHEMBL29097 IC50 > 10.0 nM -
CHEMBL16596 QUIFLAPON IC50 > 10000.0 nM -