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Target
Histamine H3 receptor
Ligand
BDBM50297734
Substrate
n/a
Meas. Tech.
ChEMBL_584028 (CHEMBL1055908)
Ki
30±n/a nM
Citation
 Rodríguez Sarmiento, RM; Nettekoven, MH; Taylor, S; Plancher, JM; Richter, H; Roche, O Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs. Bioorg Med Chem Lett 19:4495-500 (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:
BDBM50297734
Synonyms:
(6-((1S,6S)-7-isopropyl-7-azabicyclo[4.1.1]octan-3-yloxy)quinolin-2-yl)(morpholino)methanone | CHEMBL558465
Type:
Small organic molecule
Emp. Form.:
C24H31N3O3
Mol. Mass.:
409.5212
SMILES:
CC(C)N1[C@@H]2C[C@H]1CC(CC2)Oc1ccc2nc(ccc2c1)C(=O)N1CCOCC1 |r,TLB:1:3:8.9.10.7:5|
Structure:
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