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Assay Detail

CHEMBL1787316

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

Functional
Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type L6
Confidence 1 — Organism
Curated By Autocuration

Target

L6 (CHEMBL614793)
Type CELL-LINE
Organism Rattus norvegicus

Publication

Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.
Pfefferkorn JA, Litchfield J, Hutchings R, Cheng XM, Larsen SD, Auerbach B, Bush MR, Lee C, Erasga N, Bowles DM, Boyles DC, Lu G, Sekerke C, Askew V, Hanselman JC, Dillon L, Lin Z, Robertson A, Olsen K, Boustany C, Atkinson K, Goosen TC, Sahasrabudhe V, Chupka J, Duignan DB, Feng B, Scialis R, Kimoto E, Bi YA, Lai Y, El-Kattan A, Bakker-Arkema R, Barclay P, Kindt E, Le V, Mandema JW, Milad M, Tait BD, Kennedy R, Trivedi BK, Kowala M.
Bioorg Med Chem Lett (2011) 21 : 2725 -2731
PubMed 21183342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.85 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782552 1 6.75
CHEMBL1782562 1 6.65
CHEMBL1496 ROSUVASTATIN 4.0 1 6.60
CHEMBL1782559 1 6.35
CHEMBL1782553 1 6.27
CHEMBL1782556 1 6.27
CHEMBL1782551 1 6.20
CHEMBL251188 1 6.14
CHEMBL1782563 1 6.05
CHEMBL1782558 1 5.79
CHEMBL1782560 1 5.56
CHEMBL1782550 1 5.52
CHEMBL1782554 1 5.31
CHEMBL1782561 1 5.31
CHEMBL1782555 1 5.19
CHEMBL1782557 1 4.97
CHEMBL1782062 1 4.57
CHEMBL1782564 1 -
CHEMBL1782565 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782552 IC50 = 178.0 nM 6.75
CHEMBL1782562 IC50 = 224.0 nM 6.65
CHEMBL1496 ROSUVASTATIN IC50 = 250.0 nM 6.60
CHEMBL1782559 IC50 = 444.0 nM 6.35
CHEMBL1782553 IC50 = 532.0 nM 6.27
CHEMBL1782556 IC50 = 538.0 nM 6.27
CHEMBL1782551 IC50 = 632.0 nM 6.20
CHEMBL251188 IC50 = 730.0 nM 6.14
CHEMBL1782563 IC50 = 890.0 nM 6.05
CHEMBL1782558 IC50 = 1620.0 nM 5.79
CHEMBL1782560 IC50 = 2780.0 nM 5.56
CHEMBL1782550 IC50 = 3030.0 nM 5.52
CHEMBL1782554 IC50 = 4850.0 nM 5.31
CHEMBL1782561 IC50 = 4870.0 nM 5.31
CHEMBL1782555 IC50 = 6400.0 nM 5.19
CHEMBL1782557 IC50 = 10700.0 nM 4.97
CHEMBL1782062 IC50 = 27200.0 nM 4.57
CHEMBL1782564 IC50 > 100000.0 nM -
CHEMBL1782565 IC50 > 100000.0 nM -