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Target
Histamine H1 receptor
Ligand
BDBM50191289
Substrate
n/a
Meas. Tech.
ChEMBL_556998 (CHEMBL960689)
Ki
7.76±n/a nM
Citation
 Smits, RA; de Esch, IJ; Zuiderveld, OP; Broeker, J; Sansuk, K; Guaita, E; Coruzzi, G; Adami, M; Haaksma, E; Leurs, R Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem 51:7855-65 (2008) [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:
BDBM50191289
Synonyms:
7-chloro-11-(4-methyl-piperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine | CHEMBL213912 | VUF-6884
Type:
Small organic molecule
Emp. Form.:
C18H18ClN3O
Mol. Mass.:
327.808
SMILES:
CN1CCN(CC1)C1=Nc2ccc(Cl)cc2Oc2ccccc12 |t:8|
Structure:
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