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Assay Detail

CHEMBL619245

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

Binding
Iin vitro inhibition of 5-lipoxygenase activity in rat basophil leukemia type 1(RBL1) cell homogenates, (reduction of [14C]-5-HETE formation)
23
Total Activities
23
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 (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.
Malleron JL, Roussel G, Gueremy G, Ponsinet G, Robin JL, Terlain B, Tissieres JM.
J Med Chem (1990) 33 : 2744 -2749
PubMed 2213827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.59 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50 QUERCETIN 3.0 1 6.40
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 6.30
CHEMBL8562 1 6.22
CHEMBL92758 1 6.05
CHEMBL93310 1 6.00
CHEMBL91981 1 6.00
CHEMBL93670 1 5.96
CHEMBL93599 1 5.70
CHEMBL316996 1 5.70
CHEMBL313860 1 5.70
CHEMBL274642 BW-755C 1 5.70
CHEMBL8425 NAFAZATROM 2.0 1 5.60
CHEMBL329606 1 5.60
CHEMBL93598 1 5.46
CHEMBL91004 1 5.30
CHEMBL93046 1 4.30
CHEMBL91982 1 4.30
CHEMBL413482 1 4.30
CHEMBL273584 1 -
CHEMBL328432 1 -
CHEMBL94042 1 -
CHEMBL94220 1 -
CHEMBL432054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50 QUERCETIN IC50 = 400.0 nM 6.40
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 500.0 nM 6.30
CHEMBL8562 IC50 = 600.0 nM 6.22
CHEMBL92758 IC50 = 900.0 nM 6.05
CHEMBL93310 IC50 = 1000.0 nM 6.00
CHEMBL91981 IC50 = 1000.0 nM 6.00
CHEMBL93670 IC50 = 1100.0 nM 5.96
CHEMBL93599 IC50 = 2000.0 nM 5.70
CHEMBL316996 IC50 = 2000.0 nM 5.70
CHEMBL313860 IC50 = 2000.0 nM 5.70
CHEMBL274642 BW-755C IC50 = 2000.0 nM 5.70
CHEMBL8425 NAFAZATROM IC50 = 2500.0 nM 5.60
CHEMBL329606 IC50 = 2500.0 nM 5.60
CHEMBL93598 IC50 = 3500.0 nM 5.46
CHEMBL91004 IC50 = 5000.0 nM 5.30
CHEMBL93046 IC50 = 50000.0 nM 4.30
CHEMBL91982 IC50 = 50000.0 nM 4.30
CHEMBL413482 IC50 = 50000.0 nM 4.30
CHEMBL273584 IC50 > 50000.0 nM -
CHEMBL328432 IC50 > 50000.0 nM -
CHEMBL94042 IC50 > 50000.0 nM -
CHEMBL94220 IC50 > 50000.0 nM -
CHEMBL432054 IC50 > 50000.0 nM -