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Target
Histamine H1 receptor
Ligand
BDBM22875
Substrate
n/a
Meas. Tech.
ChEMBL_1760112 (CHEMBL4195120)
Ki
2.0±n/a nM
Citation
 Pa?czyk, K; Pytka, K; Jakubczyk, M; Rapacz, A; Sa?at, K; Furga?a, A; Siwek, A; G?uch-Lutwin, M; Grybo?, A; S?oczy?ska, K; P?kala, E; ?mudzki, P; Bucki, A; Ko?aczkowski, M; ?elaszczyk, D; Marona, H; Waszkielewicz, AM Synthesis and activity of di- or trisubstituted N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives on the central nervous system. Bioorg Med Chem Lett 28:2039-2049 (2018) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM22875
Synonyms:
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethan-1-ol | Atarax | CHEMBL896 | Durrax | Hydroxyzine | Hydroxyzine Pamoate | Hydroxyzine, (R) | Orgatrax | Vistaril | med.21724, Compound 187
Type:
Small organic molecule
Emp. Form.:
C21H27ClN2O2
Mol. Mass.:
374.904
SMILES:
OCCOCCN1CCN(CC1)C(c1ccccc1)c1ccc(Cl)cc1
Structure:
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