Target
Histamine H3 receptor
Ligand
BDBM50276073
Substrate
n/a
Meas. Tech.
ChEMBL_493066 (CHEMBL937681)
EC50
1.64±n/a nM
Citation
 Ghorai, PKraus, AKeller, MGötte, CIgel, PSchneider, ESchnell, DBernhardt, GDove, SZabel, MElz, SSeifert, RBuschauer, A Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine H2 receptor agonists. J Med Chem 51:7193-204 (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:
BDBM50276073
Synonyms:
CHEMBL502339 | N1-[3-(1H-Imidazol-4-yl)propyl]-N2-[3-(thiophen-2-yl)butanoyl] guanidine
Type:
Small organic molecule
Emp. Form.:
C15H21N5OS
Mol. Mass.:
319.425
SMILES:
CC(CC(=O)NC(N)=NCCCc1cnc[nH]1)c1cccs1 |w:8.8|
Structure:
Search PDB for entries with ligand similarity: