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Target
Histamine H1 receptor
Ligand
BDBM50017696
Substrate
n/a
Meas. Tech.
ChEMBL_1275661 (CHEMBL3090832)
IC50
5.4±n/a nM
Citation
 Peters, JU Polypharmacology - foe or friend? J Med Chem 56:8955-71 (2013) [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:
BDBM50017696
Synonyms:
(2-dimethylamino-2-methyl)ethyl-N-dibenzoparathiazine | 10-(2-Dimethylaminopropyl)phenothiazine | 10-[2-(dimethylamino)propyl]phenothiazine | CHEMBL643 | N,N,alpha-trimethyl-10H-phenothiazine-10-ethanamine | N,N-dimethyl-1-(10H-phenothiazin-10-yl)propan-2-amine | PROMETHAZINE | med.21724, Compound 16 | proazamine
Type:
Small organic molecule
Emp. Form.:
C17H20N2S
Mol. Mass.:
284.419
SMILES:
CC(CN1c2ccccc2Sc2ccccc12)N(C)C
Structure:
Search PDB for entries with ligand similarity: