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Assay Detail

CHEMBL661652

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

Binding
Inhibition of recombinant human CETP-mediated transfer of [3H]CE from HDL to LDL
14
Total Activities
14
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

Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
Durley RC, Grapperhaus ML, Massa MA, Mischke DA, Parnas BL, Fobian YM, Rath NP, Honda DD, Zeng M, Connolly DT, Heuvelman DM, Witherbee BJ, Glenn KC, Krul ES, Smith ME, Sikorski JA.
J Med Chem (2000) 43 : 4575 -4578
PubMed 11101348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.52 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303954 1 7.70
CHEMBL297971 1 6.70
CHEMBL340310 1 6.10
CHEMBL127895 1 6.00
CHEMBL127319 1 5.40
CHEMBL126074 1 5.30
CHEMBL338797 1 4.92
CHEMBL127187 1 4.82
CHEMBL143959 1 4.82
CHEMBL421654 1 4.60
CHEMBL125473 1 4.40
CHEMBL126544 1 -
CHEMBL126972 1 -
CHEMBL126775 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303954 IC50 = 20.0 nM 7.70
CHEMBL297971 IC50 = 200.0 nM 6.70
CHEMBL340310 IC50 = 800.0 nM 6.10
CHEMBL127895 IC50 = 1000.0 nM 6.00
CHEMBL127319 IC50 = 4000.0 nM 5.40
CHEMBL126074 IC50 = 5000.0 nM 5.30
CHEMBL338797 IC50 = 12000.0 nM 4.92
CHEMBL127187 IC50 = 15000.0 nM 4.82
CHEMBL143959 IC50 = 15000.0 nM 4.82
CHEMBL421654 IC50 = 25000.0 nM 4.60
CHEMBL125473 IC50 = 40000.0 nM 4.40
CHEMBL126544 IC50 > 100000.0 nM -
CHEMBL126972 IC50 > 100000.0 nM -
CHEMBL126775 IC50 > 100000.0 nM -