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Target
Histamine H1 receptor
Ligand
BDBM506776
Substrate
n/a
Meas. Tech.
H1 and 5-HT2A Binding Assay
Ki
37.5±n/a nM
Citation
 Duggan, ME; Edgar, DM Piperazine substituted azapine derivatives and uses thereof US Patent  US11046651 Publication Date 6/29/2021 
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:
BDBM506776
Synonyms:
US11046651, Compound 3
Type:
Small organic molecule
Emp. Form.:
C24H28ClN3O3
Mol. Mass.:
441.95
SMILES:
CCc1ccc2c(Oc3cc(Cl)ccc3N=C2N2CCN(CC(C)(C)C(O)=O)CC2)c1 |c:16|
Structure:
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