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Assay Detail

CHEMBL944784

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Functional
Inhibition of cholesterol synthesis in rat hepatocyte
26
Total Activities
26
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

Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors.
Park WK, Kennedy RM, Larsen SD, Miller S, Roth BD, Song Y, Steinbaugh BA, Sun K, Tait BD, Kowala MC, Trivedi BK, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu GH, Robertson A, Sekerke C.
Bioorg Med Chem Lett (2008) 18 : 1151 -1156
PubMed 18155906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 9.00 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438884 1 9.66
CHEMBL403430 1 9.60
CHEMBL1496 ROSUVASTATIN 4.0 1 9.57
CHEMBL252855 1 9.43
CHEMBL252854 1 9.40
CHEMBL437790 1 9.35
CHEMBL437795 1 9.33
CHEMBL429487 1 9.30
CHEMBL403646 1 9.24
CHEMBL437783 1 9.17
CHEMBL404672 1 9.16
CHEMBL253055 1 9.12
CHEMBL401949 1 9.10
CHEMBL252657 1 9.02
CHEMBL1487 ATORVASTATIN 4.0 1 9.00
CHEMBL253054 1 8.96
CHEMBL1064 SIMVASTATIN 4.0 1 8.89
CHEMBL401950 1 8.85
CHEMBL1477 CERIVASTATIN 4.0 1 8.77
CHEMBL404671 1 8.74
CHEMBL251863 1 8.60
CHEMBL253258 1 8.57
CHEMBL402622 1 8.52
CHEMBL253053 1 8.48
CHEMBL265899 1 8.30
CHEMBL1144 PRAVASTATIN 4.0 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438884 IC50 = 0.22 nM 9.66
CHEMBL403430 IC50 = 0.25 nM 9.60
CHEMBL1496 ROSUVASTATIN IC50 = 0.27 nM 9.57
CHEMBL252855 IC50 = 0.37 nM 9.43
CHEMBL252854 IC50 = 0.4 nM 9.40
CHEMBL437790 IC50 = 0.45 nM 9.35
CHEMBL437795 IC50 = 0.47 nM 9.33
CHEMBL429487 IC50 = 0.5 nM 9.30
CHEMBL403646 IC50 = 0.57 nM 9.24
CHEMBL437783 IC50 = 0.67 nM 9.17
CHEMBL404672 IC50 = 0.69 nM 9.16
CHEMBL253055 IC50 = 0.75 nM 9.12
CHEMBL401949 IC50 = 0.8 nM 9.10
CHEMBL252657 IC50 = 0.96 nM 9.02
CHEMBL1487 ATORVASTATIN IC50 = 0.99 nM 9.00
CHEMBL253054 IC50 = 1.1 nM 8.96
CHEMBL1064 SIMVASTATIN IC50 = 1.3 nM 8.89
CHEMBL401950 IC50 = 1.4 nM 8.85
CHEMBL1477 CERIVASTATIN IC50 = 1.7 nM 8.77
CHEMBL404671 IC50 = 1.8 nM 8.74
CHEMBL251863 IC50 = 2.5 nM 8.60
CHEMBL253258 IC50 = 2.7 nM 8.57
CHEMBL402622 IC50 = 3.0 nM 8.52
CHEMBL253053 IC50 = 3.3 nM 8.48
CHEMBL265899 IC50 = 5.0 nM 8.30
CHEMBL1144 PRAVASTATIN IC50 = 17.0 nM 7.77