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Target
Histamine H3 receptor
Ligand
BDBM22541
Substrate
n/a
Meas. Tech.
ChEMBL_576568 (CHEMBL1034549)
Ki
3.16±n/a nM
Citation
 Lim, HD; Istyastono, EP; van de Stolpe, A; Romeo, G; Gobbi, S; Schepers, M; Lahaye, R; Menge, WM; Zuiderveld, OP; Jongejan, A; Smits, RA; Bakker, RA; Haaksma, EE; Leurs, R; de Esch, IJ Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: synthesis, pharmacological evaluation, and cross-target QSAR studies. Bioorg Med Chem 17:3987-94 (2009) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48691.47
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM22541
Synonyms:
Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H-imidazol-5-yl)propyl]sulfanyl}methanimidamide | VUF 9153 | VUF-9153 | VUF9153
Type:
Small organic molecule
Emp. Form.:
C14H17ClN4S
Mol. Mass.:
308.83
SMILES:
NC(SCCCc1cnc[nH]1)=NCc1ccc(Cl)cc1 |w:11.12|
Structure:
Search PDB for entries with ligand similarity: