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Assay Detail

CHEMBL4132566

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

Binding
Inhibition of recombinant human CETP after 3 hrs using fluorescent cholesteryl containing HDL after 3 hrs by fluorescence assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
Chen D, Huang X, Zhou H, Luo H, Wang P, Chang Y, He X, Ni S, Shen Q, Cao G, Sun H, Wen X, Liu J.
Eur J Med Chem (2017) 139 : 201 -213
PubMed 28802120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.13 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800807 ANACETRAPIB 3.0 1 7.47
CHEMBL502586 1 5.64
CHEMBL509269 1 5.47
CHEMBL320364 1 5.46
CHEMBL446073 OLEANOLIC ACID 3-O-SUCCINATE 1 5.37
CHEMBL4168273 1 5.16
CHEMBL4168563 1 4.99
CHEMBL4175055 1 4.64
CHEMBL1171266 1 4.42
CHEMBL4164042 1 4.41
CHEMBL169 URSOLIC ACID 2.0 1 4.33
CHEMBL2347257 1 4.16
CHEMBL4163502 1 -
CHEMBL4174842 1 -
CHEMBL4166950 1 -
CHEMBL2347261 1 -
CHEMBL2347262 1 -
CHEMBL2347265 1 -
CHEMBL168 OLEANOLIC_ACID 1 -
CHEMBL486822 ACETYL OLEANOLIC ACID 1 -
CHEMBL4171609 1 -
CHEMBL4162241 1 -
CHEMBL4170152 1 -
CHEMBL4165145 1 -
CHEMBL4175751 1 -
CHEMBL4161713 1 -
CHEMBL4172342 1 -
CHEMBL4171915 1 -
CHEMBL4159725 1 -
CHEMBL269277 BETULINIC ACID 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800807 ANACETRAPIB IC50 = 33.8 nM 7.47
CHEMBL502586 IC50 = 2300.0 nM 5.64
CHEMBL509269 IC50 = 3400.0 nM 5.47
CHEMBL320364 IC50 = 3500.0 nM 5.46
CHEMBL446073 OLEANOLIC ACID 3-O-SUCCINATE IC50 = 4300.0 nM 5.37
CHEMBL4168273 IC50 = 7000.0 nM 5.16
CHEMBL4168563 IC50 = 10300.0 nM 4.99
CHEMBL4175055 IC50 = 23100.0 nM 4.64
CHEMBL1171266 IC50 = 38000.0 nM 4.42
CHEMBL4164042 IC50 = 38900.0 nM 4.41
CHEMBL169 URSOLIC ACID IC50 = 46600.0 nM 4.33
CHEMBL2347257 IC50 = 68500.0 nM 4.16
CHEMBL3126476 IC50 - -
CHEMBL4163502 IC50 - -
CHEMBL4174842 IC50 - -
CHEMBL4166950 IC50 - -
CHEMBL2347261 IC50 - -
CHEMBL2347262 IC50 - -
CHEMBL2347265 IC50 - -
CHEMBL168 OLEANOLIC_ACID IC50 - -
CHEMBL486822 ACETYL OLEANOLIC ACID IC50 - -
CHEMBL4171609 IC50 - -
CHEMBL4162241 IC50 - -
CHEMBL4170152 IC50 - -
CHEMBL4165145 IC50 - -
CHEMBL4175751 IC50 - -
CHEMBL4161713 IC50 - -
CHEMBL4172342 IC50 - -
CHEMBL4171915 IC50 - -
CHEMBL4159725 IC50 - -
CHEMBL269277 BETULINIC ACID IC50 - -