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Target
Histamine H3 receptor
Ligand
BDBM50341448
Substrate
n/a
Meas. Tech.
ChEMBL_1628378 (CHEMBL3870963)
Ki
148±n/a nM
Citation
 Procopiou, PA; Ancliff, RA; Gore, PM; Hancock, AP; Hodgson, ST; Holmes, DS; Keeling, SP; Looker, BE; Parr, NA; Rowedder, JE; Slack, RJ The discovery of quinoline based single-ligand human H Bioorg Med Chem Lett 26:5855-5859 (2016) [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:
BDBM50341448
Synonyms:
4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one | AZELASTINE | Astelin | Astepro | CHEMBL639 | Optilast | Optivar | Rhinolast | US20230414632, Compound II-a | rac-Azelastine
Type:
Small organic molecule
Emp. Form.:
C22H24ClN3O
Mol. Mass.:
381.898
SMILES:
CN1CCCC(CC1)n1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
Structure:
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