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Assay Detail

CHEMBL808971

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

Binding
In vitro inhibition against rat microsomal squalene synthase (SS)
43
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and activity of a novel series of 3-biarylquinuclidine squalene synthase inhibitors.
Brown GR, Clarke DS, Foubister AJ, Freeman S, Harrison PJ, Johnson MC, Mallion KB, McCormick J, McTaggart F, Reid AC, Smith GJ, Taylor MJ.
J Med Chem (1996) 39 : 2971 -2979
PubMed 8709131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.20 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317462 1 8.52
CHEMBL327957 1 8.40
CHEMBL322868 1 8.30
CHEMBL100506 1 8.22
CHEMBL322662 1 8.15
CHEMBL279261 3 8.15
CHEMBL319172 1 8.10
CHEMBL319077 1 7.96
CHEMBL101492 1 7.89
CHEMBL100727 1 7.75
CHEMBL100392 1 7.75
CHEMBL99626 1 7.68
CHEMBL99679 1 7.57
CHEMBL316713 1 7.52
CHEMBL99839 1 7.52
CHEMBL329766 1 7.40
CHEMBL327738 1 7.22
CHEMBL319389 1 7.22
CHEMBL419899 1 7.22
CHEMBL100912 1 7.16
CHEMBL100913 1 6.88
CHEMBL329516 1 6.85
CHEMBL100691 1 6.79
CHEMBL317316 1 6.72
CHEMBL100180 1 6.70
CHEMBL316840 1 6.62
CHEMBL322664 1 6.57
CHEMBL329513 1 6.43
CHEMBL318301 1 6.24
CHEMBL319594 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317462 IC50 = 3.0 nM 8.52
CHEMBL327957 IC50 = 4.0 nM 8.40
CHEMBL322868 IC50 = 5.0 nM 8.30
CHEMBL100506 IC50 = 6.0 nM 8.22
CHEMBL279261 IC50 = 7.0 nM 8.15
CHEMBL322662 IC50 = 7.0 nM 8.15
CHEMBL319172 IC50 = 8.0 nM 8.10
CHEMBL319077 IC50 = 11.0 nM 7.96
CHEMBL101492 IC50 = 13.0 nM 7.89
CHEMBL279261 IC50 = 16.0 nM 7.80
CHEMBL100727 IC50 = 18.0 nM 7.75
CHEMBL100392 IC50 = 18.0 nM 7.75
CHEMBL99626 IC50 = 21.0 nM 7.68
CHEMBL99679 IC50 = 27.0 nM 7.57
CHEMBL316713 IC50 = 30.0 nM 7.52
CHEMBL99839 IC50 = 30.0 nM 7.52
CHEMBL329766 IC50 = 40.0 nM 7.40
CHEMBL327738 IC50 = 60.0 nM 7.22
CHEMBL319389 IC50 = 60.0 nM 7.22
CHEMBL419899 IC50 = 60.0 nM 7.22
CHEMBL100912 IC50 = 70.0 nM 7.16
CHEMBL279261 IC50 = 121.0 nM 6.92
CHEMBL100913 IC50 = 132.0 nM 6.88
CHEMBL329516 IC50 = 140.0 nM 6.85
CHEMBL100691 IC50 = 161.0 nM 6.79
CHEMBL317316 IC50 = 190.0 nM 6.72
CHEMBL100180 IC50 = 200.0 nM 6.70
CHEMBL316840 IC50 = 240.0 nM 6.62
CHEMBL322664 IC50 = 270.0 nM 6.57
CHEMBL329513 IC50 = 370.0 nM 6.43
CHEMBL318301 IC50 = 580.0 nM 6.24
CHEMBL319594 IC50 = 1200.0 nM 5.92
CHEMBL101863 IC50 = 2500.0 nM 5.60
CHEMBL101863 IC50 = 2500.0 nM 5.60
CHEMBL55300 IC50 = 30000.0 nM 4.52
CHEMBL102110 IC50 > 2500.0 nM -
CHEMBL101283 IC50 > 2500.0 nM -
CHEMBL102958 IC50 > 2500.0 nM -
CHEMBL100396 IC50 > 2500.0 nM -
CHEMBL102188 IC50 > 2500.0 nM -
CHEMBL98414 IC50 > 2500.0 nM -
CHEMBL97873 IC50 > 2500.0 nM -
CHEMBL103895 IC50 > 2500.0 nM -