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Assay Detail

CHEMBL781694

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

Functional
In vitro inhibition of LTB4 production was measured in rat blood
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
Bruneau P, Delvare C, Edwards MP, McMillan RM.
J Med Chem (1991) 34 : 1028 -1036
PubMed 1848292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.66 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3144716 1 6.57
CHEMBL1719803 1 6.51
CHEMBL1984519 1 6.44
CHEMBL3144717 1 6.40
CHEMBL3144578 1 6.27
CHEMBL3144586 1 6.26
CHEMBL3144719 1 6.21
CHEMBL3144714 1 6.11
CHEMBL3144577 1 6.01
CHEMBL3144584 1 6.00
CHEMBL3144574 1 5.96
CHEMBL3144583 1 5.89
CHEMBL3144575 1 5.85
CHEMBL3144582 1 5.85
CHEMBL3144579 1 5.82
CHEMBL3144722 1 5.75
CHEMBL3144715 1 5.75
CHEMBL276725 1 5.70
CHEMBL3144718 1 5.62
CHEMBL3144573 1 5.60
CHEMBL3144720 1 5.58
CHEMBL8747 REV-5901 1 5.52
CHEMBL3144576 1 5.52
CHEMBL412905 1 5.52
CHEMBL3144580 1 5.51
CHEMBL8612 1 5.47
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 5.30
CHEMBL8260 BAICALEIN 2.0 1 5.00
CHEMBL7660 PHENIDONE 1 5.00
CHEMBL50 QUERCETIN 3.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3144716 IC50 = 270.0 nM 6.57
CHEMBL1719803 IC50 = 310.0 nM 6.51
CHEMBL1984519 IC50 = 360.0 nM 6.44
CHEMBL3144717 IC50 = 400.0 nM 6.40
CHEMBL3144578 IC50 = 540.0 nM 6.27
CHEMBL3144586 IC50 = 550.0 nM 6.26
CHEMBL3144719 IC50 = 610.0 nM 6.21
CHEMBL3144714 IC50 = 780.0 nM 6.11
CHEMBL3144577 IC50 = 970.0 nM 6.01
CHEMBL3144584 IC50 = 1000.0 nM 6.00
CHEMBL3144574 IC50 = 1100.0 nM 5.96
CHEMBL3144583 IC50 = 1300.0 nM 5.89
CHEMBL3144575 IC50 = 1400.0 nM 5.85
CHEMBL3144582 IC50 = 1400.0 nM 5.85
CHEMBL3144579 IC50 = 1500.0 nM 5.82
CHEMBL3144722 IC50 = 1800.0 nM 5.75
CHEMBL3144715 IC50 = 1800.0 nM 5.75
CHEMBL276725 IC50 = 2000.0 nM 5.70
CHEMBL3144718 IC50 = 2400.0 nM 5.62
CHEMBL3144573 IC50 = 2500.0 nM 5.60
CHEMBL3144720 IC50 = 2600.0 nM 5.58
CHEMBL3144576 IC50 = 3000.0 nM 5.52
CHEMBL412905 IC50 = 3000.0 nM 5.52
CHEMBL8747 REV-5901 IC50 = 3000.0 nM 5.52
CHEMBL3144580 IC50 = 3100.0 nM 5.51
CHEMBL8612 IC50 = 3400.0 nM 5.47
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 5000.0 nM 5.30
CHEMBL8260 BAICALEIN IC50 = 10000.0 nM 5.00
CHEMBL7660 PHENIDONE IC50 = 10000.0 nM 5.00
CHEMBL50 QUERCETIN IC50 = 10000.0 nM 5.00
CHEMBL3144581 IC50 = 11000.0 nM 4.96
CHEMBL274642 BW-755C IC50 = 20000.0 nM 4.70
CHEMBL274403 IC50 = 30000.0 nM 4.52
CHEMBL8425 NAFAZATROM IC50 = 50000.0 nM 4.30
CHEMBL3144723 IC50 < 1000.0 nM -
CHEMBL3144587 IC50 < 1000.0 nM -
CHEMBL268241 IC50 > 30000.0 nM -
CHEMBL8289 IC50 > 30000.0 nM -
CHEMBL276476 IC50 > 30000.0 nM -
CHEMBL8099 IC50 > 30000.0 nM -