Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM582575
Substrate
n/a
Meas. Tech.
competitive radioligand displacement and functional assays
Ki
0.50±n/a nM
Citation
 Raymond, B SEROTONIN 5-HT2A, 5-HT2B, AND 5-HT2C RECEPTOR INVERSE AGONISTS WIPO 0:0 (2023) [PubMed] 
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:
BDBM582575
Synonyms:
WO2023288027, Cmpd 2f(2S,4R)
Type:
Small organic molecule
Emp. Form.:
C24H25N
Mol. Mass.:
327.462
SMILES:
CN(C)[C@H]1C[C@H](c2cccc(c2)-c2ccccc2)c2ccccc2C1 |r|
Structure:
Search PDB for entries with ligand similarity: