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Assay Detail

CHEMBL5113161

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

Binding
Inhibition of 5-LOX in human PMNL assessed as reduction in all-trans isomers of LTB4 and 5-HETE formation preincubated for 15 mins followed by A23187 addition and measured after 10 mins by RP-HPLC analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PMNL
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: <i>In Vitro</i> and <i>In Vivo</i> Anti-Inflammatory Characterization.
Cerqua I, Musella S, Peltner LK, D'Avino D, Di Sarno V, Granato E, Vestuto V, Di Matteo R, Pace S, Ciaglia T, Bilancia R, Smaldone G, Di Matteo F, Di Micco S, Bifulco G, Pepe G, Basilicata MG, Rodriquez M, Gomez-Monterrey IM, Campiglia P, Ostacolo C, Roviezzo F, Werz O, Rossi A, Bertamino A.
J Med Chem (2022) 65 : 14456 -14480
PubMed 36318728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.74 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170803 1 6.23
CHEMBL5199450 1 6.02
CHEMBL4473010 1 5.86
CHEMBL5185907 1 5.70
CHEMBL5193145 1 5.54
CHEMBL5207672 1 5.53
CHEMBL5202375 1 5.31
CHEMBL5171972 1 -
CHEMBL5173787 1 -
CHEMBL5169630 1 -
CHEMBL5185080 1 -
CHEMBL5192930 1 -
CHEMBL4534966 1 -
CHEMBL5193098 1 -
CHEMBL5184604 1 -
CHEMBL5185283 1 -
CHEMBL5184139 1 -
CHEMBL4458075 1 -
CHEMBL5174746 1 -
CHEMBL4590950 1 -
CHEMBL4449485 1 -
CHEMBL5191521 1 -
CHEMBL5197906 1 -
CHEMBL5205807 1 -
CHEMBL5204046 1 -
CHEMBL5190558 1 -
CHEMBL5197863 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170803 IC50 = 590.0 nM 6.23
CHEMBL5199450 IC50 = 950.0 nM 6.02
CHEMBL4473010 IC50 = 1380.0 nM 5.86
CHEMBL5185907 IC50 = 1980.0 nM 5.70
CHEMBL5193145 IC50 = 2900.0 nM 5.54
CHEMBL5207672 IC50 = 2930.0 nM 5.53
CHEMBL5202375 IC50 = 4870.0 nM 5.31
CHEMBL5171972 IC50 - -
CHEMBL5173787 IC50 > 10000.0 nM -
CHEMBL5169630 IC50 > 10000.0 nM -
CHEMBL5185080 IC50 > 10000.0 nM -
CHEMBL5192930 IC50 > 10000.0 nM -
CHEMBL4534966 IC50 > 10000.0 nM -
CHEMBL5193098 IC50 > 10000.0 nM -
CHEMBL5184604 IC50 > 10000.0 nM -
CHEMBL5185283 IC50 > 10000.0 nM -
CHEMBL5184139 IC50 > 10000.0 nM -
CHEMBL4458075 IC50 > 10000.0 nM -
CHEMBL5174746 IC50 > 10000.0 nM -
CHEMBL4590950 IC50 > 10000.0 nM -
CHEMBL4449485 IC50 - -
CHEMBL5191521 IC50 > 10000.0 nM -
CHEMBL5197906 IC50 > 10000.0 nM -
CHEMBL5205807 IC50 > 10000.0 nM -
CHEMBL5204046 IC50 > 10000.0 nM -
CHEMBL5190558 IC50 > 10000.0 nM -
CHEMBL5197863 IC50 > 10000.0 nM -