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TargetCytochrome P450 2D6
LigandBDBM50341448
Substrate/Competitorn/a
Meas. Tech.ChEMBL_741719 (CHEMBL1769765)
IC50 1000±n/a nM
Citation Procopiou, PABrowning, CBuckley, JMClark, KLFechner, LGore, PMHancock, APHodgson, STHolmes, DSKranz, MLooker, BEMorriss, KMParton, DLRussell, LJSlack, RJSollis, SLVile, SWatts, CJ The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis. J Med Chem54:2183-95 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cytochrome P450 2D6
Name:Cytochrome P450 2D6
Synonyms:CP2D6_HUMAN | CYP2D6 | CYP2DL1 | CYPIID6 | Cytochrome P450 2D6 (CYP2D6) | Debrisoquine 4-hydroxylase | P450-DB1
Type:Protein
Mol. Mass.:55774.82
Organism:Homo sapiens (Human)
Description:P10635
Residue:497
Sequence:
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGVTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50341448
n/a
NameBDBM50341448
Synonyms:4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one | AZELASTINE | Astelin | Astepro | CHEMBL639 | Optilast | Optivar | Rhinolast | US20230414632, Compound II-a | rac-Azelastine
TypeSmall organic molecule
Emp. Form.C22H24ClN3O
Mol. Mass.381.898
SMILESCN1CCCC(CC1)n1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
Structure
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