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TargetCytochrome P450 3A4
LigandBDBM50090462
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1498074 (CHEMBL3582528)
IC50>20000±n/a nM
Citation Lai, AKahraman, MGovek, SNagasawa, JBonnefous, CJulien, JDouglas, KSensintaffar, JLu, NLee, KJAparicio, AKaufman, JQian, JShao, GPrudente, RMoon, MJJoseph, JDDarimont, BBrigham, DGrillot, KHeyman, RRix, PJHager, JHSmith, ND Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem58:4888-904 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cytochrome P450 3A4
Name:Cytochrome P450 3A4
Synonyms:Albendazole monooxygenase | Albendazole sulfoxidase | CP3A4_HUMAN | CYP3A3 | CYP3A4 | CYPIIIA3 | CYPIIIA4 | Cytochrome P450 3A3 | Cytochrome P450 3A4 (CYP3A4) | Cytochrome P450 HLp | Nifedipine oxidase | Quinine 3-monooxygenase | Taurochenodeoxycholate 6-alpha-hydroxylase
Type:Enzyme
Mol. Mass.:57349.57
Organism:Homo sapiens (Human)
Description:n/a
Residue:503
Sequence:
MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMF
DMECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISI
AEDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYS
MDVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICV
FPREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSI
IFIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVV
NETLRLFPIAMRLERVCKKDVEINGMFIPKGVVVMIPSYALHRDPKYWTEPEKFLPERFS
KKNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLG
GLLQPEKPVVLKVESRDGTVSGA
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50090462
n/a
NameBDBM50090462
Synonyms:CHEMBL3581693
TypeSmall organic molecule
Emp. Form.C26H20ClFN2O2
Mol. Mass.446.901
SMILESCC\C(=C(\c1ccc(\C=C\C(O)=O)cc1)c1ccc2[nH]ncc2c1)c1ccc(F)cc1Cl
Structure
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