Target
Histamine H1 receptor
Ligand
BDBM50330750
Substrate
n/a
Meas. Tech.
ChEMBL_685205 (CHEMBL1287093)
Ki
50.12±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:
BDBM50330750
Synonyms:
CHEMBL1277126
Type:
Small organic molecule
Emp. Form.:
C24H25NO3
Mol. Mass.:
375.4602
SMILES:
OC(=O)C1=CCN(CC1)C1CCC2(C1)Cc1ccccc1Oc1ccccc21 |t:3|
Structure:
Search PDB for entries with ligand similarity: