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Assay Detail

CHEMBL922901

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Functional
Inhibition of cholesterol synthesis in rat hepatocyte
31
Total Activities
31
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

Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.
Pfefferkorn JA, Song Y, Sun KL, Miller SR, Trivedi BK, Choi C, Sorenson RJ, Bratton LD, Unangst PC, Larsen SD, Poel TJ, Cheng XM, Lee C, Erasga N, Auerbach B, Askew V, Dillon L, Hanselman JC, Lin Z, Lu G, Robertson A, Olsen K, Mertz T, Sekerke C, Pavlovsky A, Harris MS, Bainbridge G, Caspers N, Chen H, Eberstadt M.
Bioorg Med Chem Lett (2007) 17 : 4538 -4544
PubMed 17574412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 9.31 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437774 1 10.00
CHEMBL249906 1 10.00
CHEMBL401293 1 10.00
CHEMBL398240 1 10.00
CHEMBL250317 1 10.00
CHEMBL399315 1 10.00
CHEMBL399773 1 9.70
CHEMBL1496 ROSUVASTATIN 4.0 1 9.57
CHEMBL250953 1 9.52
CHEMBL250088 1 9.52
CHEMBL399313 1 9.52
CHEMBL399360 1 9.40
CHEMBL249724 1 9.40
CHEMBL400973 1 9.30
CHEMBL249273 1 9.30
CHEMBL400560 1 9.30
CHEMBL438694 1 9.22
CHEMBL403127 1 9.15
CHEMBL400874 1 9.15
CHEMBL249884 1 9.15
CHEMBL398551 1 9.05
CHEMBL250090 1 9.05
CHEMBL394937 1 9.00
CHEMBL399771 1 8.92
CHEMBL400747 1 8.92
CHEMBL1064 SIMVASTATIN 4.0 1 8.89
CHEMBL250749 1 8.82
CHEMBL398239 1 8.82
CHEMBL250500 1 8.80
CHEMBL250707 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437774 IC50 = 0.1 nM 10.00
CHEMBL249906 IC50 = 0.1 nM 10.00
CHEMBL401293 IC50 = 0.1 nM 10.00
CHEMBL398240 IC50 = 0.1 nM 10.00
CHEMBL250317 IC50 = 0.1 nM 10.00
CHEMBL399315 IC50 = 0.1 nM 10.00
CHEMBL399773 IC50 = 0.2 nM 9.70
CHEMBL1496 ROSUVASTATIN IC50 = 0.27 nM 9.57
CHEMBL250953 IC50 = 0.3 nM 9.52
CHEMBL250088 IC50 = 0.3 nM 9.52
CHEMBL399313 IC50 = 0.3 nM 9.52
CHEMBL399360 IC50 = 0.4 nM 9.40
CHEMBL249724 IC50 = 0.4 nM 9.40
CHEMBL400973 IC50 = 0.5 nM 9.30
CHEMBL400560 IC50 = 0.5 nM 9.30
CHEMBL249273 IC50 = 0.5 nM 9.30
CHEMBL438694 IC50 = 0.6 nM 9.22
CHEMBL403127 IC50 = 0.7 nM 9.15
CHEMBL400874 IC50 = 0.7 nM 9.15
CHEMBL249884 IC50 = 0.7 nM 9.15
CHEMBL398551 IC50 = 0.9 nM 9.05
CHEMBL250090 IC50 = 0.9 nM 9.05
CHEMBL394937 IC50 = 1.0 nM 9.00
CHEMBL399771 IC50 = 1.2 nM 8.92
CHEMBL400747 IC50 = 1.2 nM 8.92
CHEMBL1064 SIMVASTATIN IC50 = 1.3 nM 8.89
CHEMBL250749 IC50 = 1.5 nM 8.82
CHEMBL398239 IC50 = 1.5 nM 8.82
CHEMBL250500 IC50 = 1.6 nM 8.80
CHEMBL250707 IC50 = 2.0 nM 8.70
CHEMBL251499 IC50 = 4.9 nM 8.31