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Target
Histamine H3 receptor
Ligand
BDBM123510
Substrate
n/a
Meas. Tech.
ChEMBL_1744234 (CHEMBL4178744)
IC50
>30000±n/a nM
Citation
 Velcicky, J; Miltz, W; Oberhauser, B; Orain, D; Vaupel, A; Weigand, K; Dawson King, J; Littlewood-Evans, A; Nash, M; Feifel, R; Loetscher, P Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem 60:3672-3683 (2017) [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:
BDBM123510
Synonyms:
US8748435, 35
Type:
Small organic molecule
Emp. Form.:
C24H28N6O
Mol. Mass.:
416.5187
SMILES:
CCc1nn2c(C)cc(C)nc2c1Cc1ccc(cc1)-c1nnc(o1)C1CCNCC1
Structure:
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