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Assay Detail

CHEMBL4843630

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Functional
In vivo inhibition of CETP in po dosed NFR-transgenic mouse measured at 60 mins
35
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG.
J Med Chem (2021) 64 : 13215 -13258
PubMed 34375108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.74 7.28
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873397 1 7.28
CHEMBL3657473 1 7.27
CHEMBL4864513 1 7.22
CHEMBL4856674 1 7.07
CHEMBL3657526 1 7.06
CHEMBL4868133 1 7.05
CHEMBL3657543 1 7.02
CHEMBL3933320 1 7.01
CHEMBL3657525 1 6.97
CHEMBL3657524 1 6.92
CHEMBL3657528 1 6.92
CHEMBL3657529 1 6.91
CHEMBL3657527 1 6.90
CHEMBL4848777 1 6.89
CHEMBL3657519 1 6.85
CHEMBL4860512 1 6.81
CHEMBL3657542 1 6.78
CHEMBL4855997 1 6.74
CHEMBL4857594 1 6.74
CHEMBL3657536 1 6.73
CHEMBL4860432 1 6.72
CHEMBL4871292 1 6.64
CHEMBL3657522 1 6.62
CHEMBL4846038 1 6.61
CHEMBL3657502 1 6.56
CHEMBL3657501 1 6.37
CHEMBL4865918 1 6.37
CHEMBL3657540 1 6.25
CHEMBL4856800 1 6.21
CHEMBL3657505 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873397 IC50 = 53.0 nM 7.28
CHEMBL3657473 IC50 = 54.0 nM 7.27
CHEMBL4864513 IC50 = 60.0 nM 7.22
CHEMBL4856674 IC50 = 85.0 nM 7.07
CHEMBL3657526 IC50 = 87.0 nM 7.06
CHEMBL4868133 IC50 = 89.0 nM 7.05
CHEMBL3657543 IC50 = 95.0 nM 7.02
CHEMBL3933320 IC50 = 97.0 nM 7.01
CHEMBL3657525 IC50 = 106.0 nM 6.97
CHEMBL3657524 IC50 = 120.0 nM 6.92
CHEMBL3657528 IC50 = 120.0 nM 6.92
CHEMBL3657529 IC50 = 124.0 nM 6.91
CHEMBL3657527 IC50 = 126.0 nM 6.90
CHEMBL4848777 IC50 = 128.0 nM 6.89
CHEMBL3657519 IC50 = 141.0 nM 6.85
CHEMBL4860512 IC50 = 154.0 nM 6.81
CHEMBL3657542 IC50 = 167.0 nM 6.78
CHEMBL4855997 IC50 = 182.0 nM 6.74
CHEMBL4857594 IC50 = 184.0 nM 6.74
CHEMBL3657536 IC50 = 188.0 nM 6.73
CHEMBL4860432 IC50 = 191.0 nM 6.72
CHEMBL4871292 IC50 = 229.0 nM 6.64
CHEMBL3657522 IC50 = 242.0 nM 6.62
CHEMBL4846038 IC50 = 246.0 nM 6.61
CHEMBL3657502 IC50 = 276.0 nM 6.56
CHEMBL4865918 IC50 = 427.0 nM 6.37
CHEMBL3657501 IC50 = 432.0 nM 6.37
CHEMBL3657540 IC50 = 560.0 nM 6.25
CHEMBL4856800 IC50 = 614.0 nM 6.21
CHEMBL3657505 IC50 = 714.0 nM 6.15
CHEMBL3657535 IC50 = 750.0 nM 6.12
CHEMBL3657541 IC50 = 860.0 nM 6.07
CHEMBL3657523 IC50 - -
CHEMBL4878757 Activity = 0.9 uM -
CHEMBL4875851 Activity = 1.4 uM -