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Assay Detail

CHEMBL665926

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Binding
Inhibition of cholesteryl ester transfer protein in presence of human serum
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cholesteryl ester transfer protein (CHEMBL3572)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein.
Durley RC, Grapperhaus ML, Hickory BS, Massa MA, Wang JL, Spangler DP, Mischke DA, Parnas BL, Fobian YM, Rath NP, Honda DD, Zeng M, Connolly DT, Heuvelman DM, Witherbee BJ, Melton MA, Glenn KC, Krul ES, Smith ME, Sikorski JA.
J Med Chem (2002) 45 : 3891 -3904
PubMed 12190312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.64 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303954 1 6.22
CHEMBL297971 1 5.25
CHEMBL339447 1 4.68
CHEMBL129412 1 4.62
CHEMBL419781 1 4.54
CHEMBL127895 1 4.40
CHEMBL129440 1 4.21
CHEMBL340407 1 4.19
CHEMBL416623 1 4.16
CHEMBL129398 1 4.16
CHEMBL421648 1 -
CHEMBL127319 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303954 IC50 = 600.0 nM 6.22
CHEMBL297971 IC50 = 5600.0 nM 5.25
CHEMBL339447 IC50 = 21000.0 nM 4.68
CHEMBL129412 IC50 = 24000.0 nM 4.62
CHEMBL419781 IC50 = 29000.0 nM 4.54
CHEMBL127895 IC50 = 40000.0 nM 4.40
CHEMBL129440 IC50 = 62000.0 nM 4.21
CHEMBL340407 IC50 = 65000.0 nM 4.19
CHEMBL416623 IC50 = 70000.0 nM 4.16
CHEMBL129398 IC50 = 70000.0 nM 4.16
CHEMBL421648 IC50 > 200000.0 nM -
CHEMBL127319 IC50 = 120000.0 nM -