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Assay Detail

CHEMBL1167052

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Binding
Inhibition of CETP in rabbit serum after 1 hr by fluorescent cholesteryl esters transfer assay
ChEMBL ↗
122
Total Activities
122
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cholesteryl ester transfer protein (CHEMBL1163116) ↗
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
Abu Khalaf R, Abu Sheikha G, Bustanji Y, Taha MO.
Eur J Med Chem (2010) 45 : 1598 -1617
PubMed 20116902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 122 6.15 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127130 — — 1 8.92
CHEMBL446661 — — 1 8.52
CHEMBL67129 — — 1 8.40
CHEMBL67117 — — 1 8.09
CHEMBL304170 — — 1 7.92
CHEMBL69699 — — 1 7.70
CHEMBL303954 — — 1 7.70
CHEMBL302797 — — 1 7.52
CHEMBL71333 — — 1 7.52
CHEMBL308436 — — 1 7.52
CHEMBL69563 — — 1 7.52
CHEMBL308019 — — 1 7.46
CHEMBL69882 — — 1 7.40
CHEMBL69415 — — 1 7.35
CHEMBL440128 — — 1 7.31
CHEMBL67055 — — 1 7.22
CHEMBL419999 — — 1 7.22
CHEMBL433103 — — 1 7.16
CHEMBL68856 — — 1 7.10
CHEMBL419437 — — 1 7.10
CHEMBL69885 — — 1 7.10
CHEMBL302352 — — 1 7.10
CHEMBL302306 — — 1 7.10
CHEMBL66503 — — 1 7.05
CHEMBL308423 — — 1 7.05
CHEMBL68722 — — 1 7.05
CHEMBL305995 — — 1 7.00
CHEMBL302786 — — 1 7.00
CHEMBL68688 — — 1 7.00
CHEMBL303472 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127130 — IC50 = 1.2 nM 8.92
CHEMBL446661 — IC50 = 3.0 nM 8.52
CHEMBL67129 — IC50 = 4.0 nM 8.40
CHEMBL67117 — IC50 = 8.1 nM 8.09
CHEMBL304170 — IC50 = 12.0 nM 7.92
CHEMBL69699 — IC50 = 20.0 nM 7.70
CHEMBL303954 — IC50 = 20.0 nM 7.70
CHEMBL302797 — IC50 = 30.0 nM 7.52
CHEMBL71333 — IC50 = 30.0 nM 7.52
CHEMBL308436 — IC50 = 30.0 nM 7.52
CHEMBL69563 — IC50 = 30.0 nM 7.52
CHEMBL308019 — IC50 = 35.0 nM 7.46
CHEMBL69882 — IC50 = 40.0 nM 7.40
CHEMBL69415 — IC50 = 45.0 nM 7.35
CHEMBL440128 — IC50 = 49.0 nM 7.31
CHEMBL67055 — IC50 = 60.0 nM 7.22
CHEMBL419999 — IC50 = 60.0 nM 7.22
CHEMBL433103 — IC50 = 70.0 nM 7.16
CHEMBL302306 — IC50 = 80.0 nM 7.10
CHEMBL68856 — IC50 = 80.0 nM 7.10
CHEMBL419437 — IC50 = 80.0 nM 7.10
CHEMBL302352 — IC50 = 80.0 nM 7.10
CHEMBL69885 — IC50 = 80.0 nM 7.10
CHEMBL68722 — IC50 = 90.0 nM 7.05
CHEMBL66503 — IC50 = 90.0 nM 7.05
CHEMBL308423 — IC50 = 90.0 nM 7.05
CHEMBL305995 — IC50 = 100.0 nM 7.00
CHEMBL302786 — IC50 = 100.0 nM 7.00
CHEMBL68688 — IC50 = 100.0 nM 7.00
CHEMBL303472 — IC50 = 100.0 nM 7.00
CHEMBL66703 — IC50 = 200.0 nM 6.70
CHEMBL67395 — IC50 = 200.0 nM 6.70
CHEMBL1163792 — IC50 = 200.0 nM 6.70
CHEMBL305003 — IC50 = 200.0 nM 6.70
CHEMBL305278 — IC50 = 200.0 nM 6.70
CHEMBL67918 — IC50 = 200.0 nM 6.70
CHEMBL68632 — IC50 = 200.0 nM 6.70
CHEMBL303937 — IC50 = 200.0 nM 6.70
CHEMBL297971 — IC50 = 200.0 nM 6.70
CHEMBL68726 — IC50 = 300.0 nM 6.52
CHEMBL67709 — IC50 = 300.0 nM 6.52
CHEMBL125629 — IC50 = 300.0 nM 6.52
CHEMBL302787 — IC50 = 300.0 nM 6.52
CHEMBL431556 — IC50 = 300.0 nM 6.52
CHEMBL68805 — IC50 = 300.0 nM 6.52
CHEMBL339447 — IC50 = 350.0 nM 6.46
CHEMBL129412 — IC50 = 390.0 nM 6.41
CHEMBL71379 — IC50 = 400.0 nM 6.40
CHEMBL67512 — IC50 = 400.0 nM 6.40
CHEMBL303833 — IC50 = 400.0 nM 6.40