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Assay Detail

CHEMBL1018362

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Functional
Inhibition of cholesterol synthesis in rat hepatocytes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Hepatocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Hepatocyte (CHEMBL613362)
Type CELL-LINE
Organism Rattus norvegicus

Publication

Thermodynamic and structure guided design of statin based inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase.
Sarver RW, Bills E, Bolton G, Bratton LD, Caspers NL, Dunbar JB, Harris MS, Hutchings RH, Kennedy RM, Larsen SD, Pavlovsky A, Pfefferkorn JA, Bainbridge G.
J Med Chem (2008) 51 : 3804 -3813
PubMed 18540668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 9.04 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL455524 1 9.92
CHEMBL488297 1 9.82
CHEMBL487632 1 9.77
CHEMBL1496 ROSUVASTATIN 4.0 1 9.64
CHEMBL504314 1 9.57
CHEMBL471745 1 9.54
CHEMBL488636 1 9.52
CHEMBL488821 1 9.51
CHEMBL488298 1 9.42
CHEMBL503128 1 9.33
CHEMBL481660 1 9.17
CHEMBL452139 1 9.10
CHEMBL520068 1 9.00
CHEMBL527431 1 8.99
CHEMBL487631 1 8.99
CHEMBL488471 1 8.94
CHEMBL471744 1 8.87
CHEMBL504300 1 8.86
CHEMBL465885 1 8.74
CHEMBL487278 1 8.63
CHEMBL488300 1 8.55
CHEMBL501917 1 8.44
CHEMBL521039 1 8.23
CHEMBL444210 1 7.86
CHEMBL488299 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL455524 IC50 = 0.12 nM 9.92
CHEMBL488297 IC50 = 0.15 nM 9.82
CHEMBL487632 IC50 = 0.17 nM 9.77
CHEMBL1496 ROSUVASTATIN IC50 = 0.23 nM 9.64
CHEMBL504314 IC50 = 0.27 nM 9.57
CHEMBL471745 IC50 = 0.29 nM 9.54
CHEMBL488636 IC50 = 0.3 nM 9.52
CHEMBL488821 IC50 = 0.31 nM 9.51
CHEMBL488298 IC50 = 0.38 nM 9.42
CHEMBL503128 IC50 = 0.47 nM 9.33
CHEMBL481660 IC50 = 0.68 nM 9.17
CHEMBL452139 IC50 = 0.802 nM 9.10
CHEMBL520068 IC50 = 0.99 nM 9.00
CHEMBL527431 IC50 = 1.03 nM 8.99
CHEMBL487631 IC50 = 1.03 nM 8.99
CHEMBL488471 IC50 = 1.16 nM 8.94
CHEMBL471744 IC50 = 1.34 nM 8.87
CHEMBL504300 IC50 = 1.37 nM 8.86
CHEMBL465885 IC50 = 1.8 nM 8.74
CHEMBL487278 IC50 = 2.34 nM 8.63
CHEMBL488300 IC50 = 2.81 nM 8.55
CHEMBL501917 IC50 = 3.63 nM 8.44
CHEMBL521039 IC50 = 5.89 nM 8.23
CHEMBL444210 IC50 = 13.9 nM 7.86
CHEMBL488299 IC50 = 26.4 nM 7.58