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Target
Histamine H3 receptor
Ligand
BDBM50315348
Substrate
n/a
Meas. Tech.
ChEMBL_625975 (CHEMBL1103494)
IC50
5800±n/a nM
Citation
 Cramp, S; Dyke, HJ; Higgs, C; Clark, DE; Gill, M; Savy, P; Jennings, N; Price, S; Lockey, PM; Norman, D; Porres, S; Wilson, F; Jones, A; Ramsden, N; Mangano, R; Leggate, D; Andersson, M; Hale, R Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett 20:2516-9 (2010) [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:
BDBM50315348
Synonyms:
(R)-8-chloro-4-(3-(methylamino)pyrrolidin-1-yl)benzofuro[3,2-d]pyrimidin-2-amine | CHEMBL1091874
Type:
Small organic molecule
Emp. Form.:
C15H16ClN5O
Mol. Mass.:
317.773
SMILES:
CN[C@@H]1CCN(C1)c1nc(N)nc2c3cc(Cl)ccc3oc12 |r|
Structure:
Search PDB for entries with ligand similarity: