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Target
Histamine H3 receptor
Ligand
BDBM50186273
Substrate
n/a
Meas. Tech.
ChEMBL_370710 (CHEMBL867233)
Ki
8.1±n/a nM
Citation
 Jesudason, CD; Beavers, LS; Cramer, JW; Dill, J; Finley, DR; Lindsley, CW; Stevens, FC; Gadski, RA; Oldham, SW; Pickard, RT; Siedem, CS; Sindelar, DK; Singh, A; Watson, BM; Hipskind, PA Synthesis and SAR of novel histamine H3 receptor antagonists. Bioorg Med Chem Lett 16:3415-8 (2006) [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:
BDBM50186273
Synonyms:
(7-(3-(piperidin-1-yl)propoxy)-3,4-dihydroisoquinolin-2(1H)-yl)(thiophen-2-yl)methanone | CHEMBL210401
Type:
Small organic molecule
Emp. Form.:
C22H28N2O2S
Mol. Mass.:
384.535
SMILES:
O=C(N1CCc2ccc(OCCCN3CCCCC3)cc2C1)c1cccs1
Structure:
Search PDB for entries with ligand similarity: