Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM35254
Substrate
n/a
Meas. Tech.
ChEMBL_84714 (CHEMBL884684)
Ki
0.3±n/a nM
Citation
Campiani, G; Butini, S; Gemma, S; Nacci, V; Fattorusso, C; Catalanotti, B; Giorgi, G; Cagnotto, A; Goegan, M; Mennini, T; Minetti, P; Di Cesare, MA; Mastroianni, D; Scafetta, N; Galletti, B; Stasi, MA; Castorina, M; Pacifici, L; Ghirardi, O; Tinti, O; Carminati, P Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. J Med Chem 45:344-59 (2002) [PubMed] Article
More Info.:
Target
Name:
Histamine H1 receptor
Synonyms:
HISTAMINE H1 | HRH1_RAT | Hrh1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55716.35
Organism:
RAT
Description:
HISTAMINE H1 HRH1 RAT::P31390
Residue:
486
Sequence:
MSFANTSSTFEDKMCEGNRTAMASPQLLPLVVVLSSISLVTVGLNLLVLYAVHSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLIMTKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLRYRTKTRASATILGAWFFSFLWVIPILGWHHFMPPAPELREDKCETDFYNVTWFKIMTAIINFYLPTLLMLWFYVKIYKAVRRHCQHRQLTNGSLPSFSELKLRSDDTKEGAKKPGRESPWGVLKRPSRDPSVGLDQKSTSEDPKMTSPTVFSQEGERETRPCFRLDIMQKQSVAEGDVRGSKANDQALSQPKMDEQSLNTCRRISETSEDQTLVDQQSFSRTTDSDTSIEPGPGRVKSRSGSNSGLDYIKITWKRLRSHSRQYVSGLHLNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKSCCSEPMHMFTIWLGYINSTLNPLIYPLCNENFKKTFKKILHIRS
Inhibitor
Name:
BDBM35254
Synonyms:
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine | CHEMBL715 | Olansek | US8802672, Olanzapine | Zyprexa | olanzapine
Type:
Small organic molecule
Emp. Form.:
C17H20N4S
Mol. Mass.:
312.432
SMILES:
CN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12 |t:8|