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TargetCholesteryl ester transfer protein
LigandBDBM138248
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2133982 (CHEMBL4843592)
IC50 213±n/a nM
Citation Vachal, PDuffy, JLCampeau, LCAmin, RPMitra, KMurphy, BAShao, PPSinclair, PJYe, FKatipally, RLu, ZOndeyka, DChen, YHZhao, KSun, WTyagarajan, SBao, JWang, SPCote, JLipardi, CMetzger, DLeung, DHartmann, GWollenberg, GKLiu, JTan, LXu, YChen, QLiu, GBlaustein, ROJohns, DG Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties. J Med Chem64:13215-13258 (2021) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cholesteryl ester transfer protein
Name:Cholesteryl ester transfer protein
Synonyms:CETP | CETP_HUMAN | Cholesteryl ester transfer protein (CETP) | Lipid transfer protein I
Type:Enzyme
Mol. Mass.:54751.53
Organism:Homo sapiens (Human)
Description:P11597
Residue:493
Sequence:
MLAATVLTLALLGNAHACSKGTSHEAGIVCRITKPALLVLNHETAKVIQTAFQRASYPDI
TGEKAMMLLGQVKYGLHNIQISHLSIASSQVELVEAKSIDVSIQNVSVVFKGTLKYGYTT
AWWLGIDQSIDFEIDSAIDLQINTQLTCDSGRVRTDAPDCYLSFHKLLLHLQGEREPGWI
KQLFTNFISFTLKLVLKGQICKEINVISNIMADFVQTRAASILSDGDIGVDISLTGDPVI
TASYLESHHKGHFIYKNVSEDLPLPTFSPTLLGDSRMLYFWFSERVFHSLAKVAFQDGRL
MLSLMGDEFKAVLETWGFNTNQEIFQEVVGGFPSQAQVTVHCLKMPKISCQNKGVVVNSS
VMVKFLFPRPDQQHSVAYTFEEDIVTTVQASYSKKKLFLSLLDFQITPKTVSNLTESSSE
SVQSFLQSMITAVGIPEVMSRLEVVFTALMNSKGVSLFDIINPEIITRDGFLLLQMDFGF
PEHLLVDFLQSLS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM138248
n/a
NameBDBM138248
Synonyms:US8871738, 31
TypeSmall organic molecule
Emp. Form.C29H25Cl2F4NO3
Mol. Mass.582.413
SMILESCOc1cc(F)c(cc1-c1ccc(cc1[C@@H]1CC[C@H]2[C@H](OC(=O)N12)c1cc(Cl)cc(Cl)c1)C(F)(F)F)C(C)C |r|
Structure
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