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Assay Detail

CHEMBL767839

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

Functional
Concentration required for 50 % inhibition of leukotriene B4 production in human PMN compared with controls in the absence of compound
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224.
Lau CK, Bélanger PC, Scheigetz J, Dufresne C, Williams HW, Maycock AL, Guindon Y, Bach T, Dallob AL, Denis D.
J Med Chem (1989) 32 : 1190 -1197
PubMed 2542553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.07 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280055 1 8.15
CHEMBL17815 1 7.96
CHEMBL18394 1 7.92
CHEMBL18946 1 7.89
CHEMBL18989 1 7.70
CHEMBL278034 1 7.70
CHEMBL18694 1 7.58
CHEMBL18820 1 7.52
CHEMBL18050 1 7.51
CHEMBL18250 1 7.34
CHEMBL18376 1 7.12
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 7.07
CHEMBL278507 1 7.00
CHEMBL18559 1 6.98
CHEMBL18536 1 6.54
CHEMBL280281 1 6.42
CHEMBL18632 1 6.24
CHEMBL280304 1 6.07
CHEMBL274233 1 5.67
CHEMBL7660 PHENIDONE 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280055 IC50 = 7.0 nM 8.15
CHEMBL17815 IC50 = 11.0 nM 7.96
CHEMBL18394 IC50 = 12.0 nM 7.92
CHEMBL18946 IC50 = 13.0 nM 7.89
CHEMBL18989 IC50 = 20.0 nM 7.70
CHEMBL278034 IC50 = 20.0 nM 7.70
CHEMBL18694 IC50 = 26.0 nM 7.58
CHEMBL18820 IC50 = 30.0 nM 7.52
CHEMBL18050 IC50 = 31.0 nM 7.51
CHEMBL18250 IC50 = 46.0 nM 7.34
CHEMBL18376 IC50 = 76.0 nM 7.12
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 85.0 nM 7.07
CHEMBL278507 IC50 = 99.0 nM 7.00
CHEMBL18559 IC50 = 105.0 nM 6.98
CHEMBL18536 IC50 = 291.0 nM 6.54
CHEMBL280281 IC50 = 376.0 nM 6.42
CHEMBL18632 IC50 = 574.0 nM 6.24
CHEMBL280304 IC50 = 860.0 nM 6.07
CHEMBL274233 IC50 = 2134.0 nM 5.67
CHEMBL7660 PHENIDONE IC50 = 9200.0 nM 5.04