Target
Histamine H1 receptor
Ligand
BDBM50416670
Substrate
n/a
Meas. Tech.
ChEMBL_651968 (CHEMBL1227641)
Ki
25.12±n/a nM
Citation
 Gianotti, MCorti, CDelle Fratte, SDi Fabio, RLeslie, CPPavone, FPiccoli, LStasi, LWigglesworth, MJ Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders. Bioorg Med Chem Lett 20:5069-73 (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:
BDBM50416670
Synonyms:
CHEMBL1222554
Type:
Small organic molecule
Emp. Form.:
C21H26N4O2
Mol. Mass.:
366.4567
SMILES:
CC(C)(CN1CCN(CC1)C1=Cc2ccccc2Cn2ccnc12)C(O)=O |t:11|
Structure:
Search PDB for entries with ligand similarity: