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Assay Detail

CHEMBL761040

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

Functional
Effect on production of LTB4 in human polymorphonuclear leukocytes
24
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid.
Hutchinson JH, Riendeau D, Brideau C, Chan C, Falgueyret JP, Guay J, Jones TR, Lépine C, Macdonald D, McFarlane CS.
J Med Chem (1994) 37 : 1153 -1164
PubMed 8164257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.78 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275634 5 8.46
CHEMBL277746 1 8.35
CHEMBL13931 1 8.30
CHEMBL16567 1 8.22
CHEMBL16285 1 8.19
CHEMBL278027 1 8.15
CHEMBL278632 1 8.15
CHEMBL279871 1 8.00
CHEMBL16244 1 7.96
CHEMBL16284 1 7.92
CHEMBL279194 1 7.82
CHEMBL16304 1 7.77
CHEMBL16389 1 7.77
CHEMBL276593 1 7.70
CHEMBL16283 1 7.51
CHEMBL16366 1 7.30
CHEMBL278478 1 7.19
CHEMBL16591 1 6.95
CHEMBL16590 1 6.70
CHEMBL16574 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275634 IC50 = 3.5 nM 8.46
CHEMBL275634 IC50 = 4.0 nM 8.40
CHEMBL277746 IC50 = 4.5 nM 8.35
CHEMBL13931 IC50 = 5.0 nM 8.30
CHEMBL16567 IC50 = 6.0 nM 8.22
CHEMBL16285 IC50 = 6.5 nM 8.19
CHEMBL275634 IC50 = 7.0 nM 8.15
CHEMBL278632 IC50 = 7.0 nM 8.15
CHEMBL278027 IC50 = 7.0 nM 8.15
CHEMBL275634 IC50 = 10.0 nM 8.00
CHEMBL279871 IC50 = 10.0 nM 8.00
CHEMBL16244 IC50 = 11.0 nM 7.96
CHEMBL16284 IC50 = 12.0 nM 7.92
CHEMBL279194 IC50 = 15.0 nM 7.82
CHEMBL275634 IC50 = 17.0 nM 7.77
CHEMBL16304 IC50 = 17.0 nM 7.77
CHEMBL16389 IC50 = 17.0 nM 7.77
CHEMBL276593 IC50 = 20.0 nM 7.70
CHEMBL16283 IC50 = 31.0 nM 7.51
CHEMBL16366 IC50 = 50.0 nM 7.30
CHEMBL278478 IC50 = 65.0 nM 7.19
CHEMBL16591 IC50 = 113.0 nM 6.95
CHEMBL16590 IC50 = 200.0 nM 6.70
CHEMBL16574 IC50 = 1100.0 nM 5.96