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Assay Detail

CHEMBL808970

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Binding
Inhibitory activity against rat liver microsomal squalene synthase was determined using [3H]FPP as radioligand
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Squalene synthase (CHEMBL3815)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.
Magnin DR, Biller SA, Chen Y, Dickson JK, Fryszman OM, Lawrence RM, Logan JV, Sieber-McMaster ES, Sulsky RB, Traeger SC, Hsieh DC, Lan SJ, Rinehart JK, Harrity TW, Jolibois KG, Kunselman LK, Rich LC, Slusarchyk DA, Ciosek CP.
J Med Chem (1996) 39 : 657 -660
PubMed 8576905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.83 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87292 1 9.15
CHEMBL348349 1 9.00
CHEMBL158707 1 8.24
CHEMBL158517 1 7.89
CHEMBL160240 1 7.82
CHEMBL160267 1 7.77
CHEMBL160318 1 7.75
CHEMBL158448 1 7.72
CHEMBL158862 1 7.46
CHEMBL158851 1 7.46
CHEMBL158978 1 7.12
CHEMBL351866 1 6.84
CHEMBL351151 1 6.77
CHEMBL158844 1 6.72
CHEMBL158527 1 6.70
CHEMBL346762 1 6.57
CHEMBL159021 1 6.54
CHEMBL158154 1 6.13
CHEMBL347175 1 5.70
CHEMBL160796 1 5.70
CHEMBL160284 1 5.34
CHEMBL158931 1 5.21
CHEMBL158667 1 5.16
CHEMBL347856 1 5.09
CHEMBL160340 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87292 IC50 = 0.7 nM 9.15
CHEMBL348349 IC50 = 1.0 nM 9.00
CHEMBL158707 IC50 = 5.7 nM 8.24
CHEMBL158517 IC50 = 13.0 nM 7.89
CHEMBL160240 IC50 = 15.0 nM 7.82
CHEMBL160267 IC50 = 17.0 nM 7.77
CHEMBL160318 IC50 = 18.0 nM 7.75
CHEMBL158448 IC50 = 19.0 nM 7.72
CHEMBL158862 IC50 = 35.0 nM 7.46
CHEMBL158851 IC50 = 35.0 nM 7.46
CHEMBL158978 IC50 = 76.0 nM 7.12
CHEMBL351866 IC50 = 144.0 nM 6.84
CHEMBL351151 IC50 = 169.0 nM 6.77
CHEMBL158844 IC50 = 192.0 nM 6.72
CHEMBL158527 IC50 = 200.0 nM 6.70
CHEMBL346762 IC50 = 268.0 nM 6.57
CHEMBL159021 IC50 = 286.0 nM 6.54
CHEMBL158154 IC50 = 740.0 nM 6.13
CHEMBL347175 IC50 = 1980.0 nM 5.70
CHEMBL160796 IC50 = 2000.0 nM 5.70
CHEMBL160284 IC50 = 4600.0 nM 5.34
CHEMBL158931 IC50 = 6200.0 nM 5.21
CHEMBL158667 IC50 = 6900.0 nM 5.16
CHEMBL347856 IC50 = 8200.0 nM 5.09
CHEMBL160340 IC50 = 14200.0 nM 4.85