Target
Histamine H1 receptor
Ligand
BDBM50402817
Substrate
n/a
Meas. Tech.
ChEMBL_887254 (CHEMBL2215810)
Ki
19.95±n/a nM
Citation
 Furber, MAlcaraz, LLuckhurst, CBahl, ABeaton, HBowers, KCollington, JDenton, RDonald, DKinchin, EMacDonald, CRigby, ARiley, RSoars, MSpringthorpe, BWebborn, P Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I. Bioorg Med Chem Lett 22:7702-6 (2012) [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:
BDBM50402817
Synonyms:
CHEMBL2208432
Type:
Small organic molecule
Emp. Form.:
C22H24Cl2N4O4
Mol. Mass.:
479.356
SMILES:
O[C@H](CNC(=O)n1c2ccccc2[nH]c1=O)CN1CCC(CC1)Oc1ccc(Cl)c(Cl)c1 |r|
Structure:
Search PDB for entries with ligand similarity: