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TargetCytochrome P450 2C8
LigandBDBM276748
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2187635 (CHEMBL5099717)
IC50>30000±n/a nM
Citation Futatsugi, KCabral, SKung, DWHuard, KLee, EBoehm, MBauman, JClark, RWCoffey, SBCrowley, CDechert-Schmitt, AMDowling, MSDullea, RGosset, JRKalgutkar, ASKou, KLi, QLian, YLoria, PMLondregan, ATNiosi, MOrozco, CPettersen, JCPfefferkorn, JAPolivkova, JRoss, TTSharma, RStock, IATesz, GWisniewska, HGoodwin, BPrice, DA Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis. J Med Chem65:15000-15013 (2022) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cytochrome P450 2C8
Name:Cytochrome P450 2C8
Synonyms:CP2C8_HUMAN | CYP2C8 | CYPIIC8 | Cytochrome P450 2C8 (CYP2C8) | P450 IIC2 | P450 MP-12/MP-20 | P450 form 1 | S-mephenytoin 4-hydroxylase
Type:Protein
Mol. Mass.:55839.23
Organism:Homo sapiens (Human)
Description:P10632
Residue:490
Sequence:
MEPFVVLVLCLSFMLLFSLWRQSCRRRKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKV
YGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRW
KEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICS
VVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALT
RSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTE
TTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSD
LVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFK
KSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLP
PSYQICFIPV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM276748
n/a
NameBDBM276748
Synonyms:US10071992, Example 3.5 | US10071992, Example 5 | US11034678, Example 5
TypeSmall organic molecule
Emp. Form.C21H23N5O4
Mol. Mass.409.4384
SMILESCCOc1cccnc1Oc1cncc(c1)-c1ncc(cn1)C(=O)NC(C)(C)CO
Structure
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