Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM22567
Substrate
n/a
Meas. Tech.
ChEMBL_1366831 (CHEMBL3297341)
Ki
1.7±n/a nM
Citation
Kolaczkowski, M; Marcinkowska, M; Bucki, A; Pawlowski, M; Mitka, K; Jaskowska, J; Kowalski, P; Kazek, G; Siwek, A; Wasik, A; Wesolowska, A; Mierzejewski, P; Bienkowski, P Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. J Med Chem 57:4543-57 (2014) [PubMed] Article
More Info.:
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:
BDBM22567
Synonyms:
3H]pyrilamine | CHEMBL511 | Dorantamin | Mepyramine | N-(4-methoxybenzyl)-N ,N -dimethyl-N-pyridin-2-ylethane-1,2-diamine | N-[2-(dimethylamino)ethyl]-N-[(4-methoxyphenyl)methyl]pyridin-2-amine | PYRILAMINE | Pyranisamine | [3H]mepyramine | [3H]pyrilamine
Type:
radiolabeled ligand
Emp. Form.:
C17H23N3O
Mol. Mass.:
285.384
SMILES:
COc1ccc(CN(CCN(C)C)c2ccccn2)cc1