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Assay Detail

CHEMBL619926

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

Binding
In vitro inhibition of 5-lipoxygenase from RBL-1 cells
35
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type RBL-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity analysis of a class of orally active hydroxamic acid inhibitors of leukotriene biosynthesis.
Summers JB, Gunn BP, Martin JG, Martin MB, Mazdiyasni H, Stewart AO, Young PR, Bouska JB, Goetze AM, Dyer RD.
J Med Chem (1988) 31 : 1960 -1964
PubMed 3172130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.22 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58810 1 6.72
CHEMBL418304 2 6.55
CHEMBL61360 1 6.54
CHEMBL58077 1 6.50
CHEMBL293413 1 6.48
CHEMBL303074 1 6.44
CHEMBL62209 1 6.43
CHEMBL59419 1 6.42
CHEMBL58866 1 6.41
CHEMBL59634 1 6.40
CHEMBL61638 1 6.39
CHEMBL58049 1 6.34
CHEMBL61608 1 6.34
CHEMBL59442 1 6.33
CHEMBL62114 1 6.30
CHEMBL58286 1 6.27
CHEMBL60231 1 6.24
CHEMBL59334 1 6.21
CHEMBL59833 1 6.21
CHEMBL58233 1 6.19
CHEMBL300346 1 6.16
CHEMBL61642 1 6.13
CHEMBL294725 1 6.12
CHEMBL61584 1 6.12
CHEMBL59250 2 6.11
CHEMBL59841 1 6.11
CHEMBL61765 1 6.06
CHEMBL58462 1 6.03
CHEMBL58212 1 5.96
CHEMBL61719 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58810 IC50 = 190.0 nM 6.72
CHEMBL418304 IC50 = 280.0 nM 6.55
CHEMBL61360 IC50 = 290.0 nM 6.54
CHEMBL58077 IC50 = 320.0 nM 6.50
CHEMBL293413 IC50 = 330.0 nM 6.48
CHEMBL303074 IC50 = 360.0 nM 6.44
CHEMBL62209 IC50 = 370.0 nM 6.43
CHEMBL418304 IC50 = 370.0 nM 6.43
CHEMBL59419 IC50 = 380.0 nM 6.42
CHEMBL58866 IC50 = 390.0 nM 6.41
CHEMBL59634 IC50 = 400.0 nM 6.40
CHEMBL61638 IC50 = 410.0 nM 6.39
CHEMBL58049 IC50 = 460.0 nM 6.34
CHEMBL61608 IC50 = 460.0 nM 6.34
CHEMBL59442 IC50 = 470.0 nM 6.33
CHEMBL62114 IC50 = 500.0 nM 6.30
CHEMBL58286 IC50 = 540.0 nM 6.27
CHEMBL60231 IC50 = 570.0 nM 6.24
CHEMBL59833 IC50 = 620.0 nM 6.21
CHEMBL59334 IC50 = 610.0 nM 6.21
CHEMBL58233 IC50 = 650.0 nM 6.19
CHEMBL300346 IC50 = 690.0 nM 6.16
CHEMBL61642 IC50 = 740.0 nM 6.13
CHEMBL61584 IC50 = 750.0 nM 6.12
CHEMBL294725 IC50 = 760.0 nM 6.12
CHEMBL59841 IC50 = 780.0 nM 6.11
CHEMBL59250 IC50 = 780.0 nM 6.11
CHEMBL59250 IC50 = 790.0 nM 6.10
CHEMBL61765 IC50 = 880.0 nM 6.06
CHEMBL58462 IC50 = 940.0 nM 6.03
CHEMBL58212 IC50 = 1100.0 nM 5.96
CHEMBL61719 IC50 = 1300.0 nM 5.89
CHEMBL441246 IC50 = 1900.0 nM 5.72
CHEMBL61862 IC50 = 2600.0 nM 5.58
CHEMBL417392 IC50 = 4900.0 nM 5.31