Target
Histamine H1 receptor
Ligand
BDBM50417363
Substrate
n/a
Meas. Tech.
ChEMBL_685205 (CHEMBL1287093)
Ki
39.81±n/a nM
Citation
 Gianotti, MBotta, MBrough, SCarletti, RCastiglioni, ECorti, CDal-Cin, MDelle Fratte, SKorajac, DLovric, MMerlo, GMesic, MPavone, FPiccoli, LRast, SRoscic, MSava, ASmehil, MStasi, LTogninelli, AWigglesworth, MJ Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders. J Med Chem 53:7778-95 (2010) [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:
BDBM50417363
Synonyms:
CHEMBL1276860
Type:
Small organic molecule
Emp. Form.:
C25H27NO2
Mol. Mass.:
373.4874
SMILES:
OC(=O)[C@@H]1[C@H]2CN(C[C@@H]12)C1CCC2(C1)Cc1ccccc1Cc1ccccc21 |r|
Structure:
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