Reaction Details |
| Report a problem with these data |
Target | Histamine H3 receptor |
---|
Ligand | BDBM50401007 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_879382 (CHEMBL2208780) |
---|
Ki | 9.3±n/a nM |
---|
Citation | Wager, TT; Pettersen, BA; Schmidt, AW; Spracklin, DK; Mente, S; Butler, TW; Howard, H; Lettiere, DJ; Rubitski, DM; Wong, DF; Nedza, FM; Nelson, FR; Rollema, H; Raggon, JW; Aubrecht, J; Freeman, JK; Marcek, JM; Cianfrogna, J; Cook, KW; James, LC; Chatman, LA; Iredale, PA; Banker, MJ; Homiski, ML; Munzner, JB; Chandrasekaran, RY Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem54:7602-20 (2011) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Histamine H3 receptor |
---|
Name: | Histamine H3 receptor |
Synonyms: | HH3R | HRH3_RAT | Hrh3 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 48607.98 |
Organism: | Rattus norvegicus (rat) |
Description: | n/a |
Residue: | 445 |
Sequence: | MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
|
|
|
BDBM50401007 |
---|
n/a |
---|
Name | BDBM50401007 |
Synonyms: | CHEMBL209478 |
Type | Small organic molecule |
Emp. Form. | C18H24N2 |
Mol. Mass. | 268.3966 |
SMILES | CN(C)Cc1ccc(cc1)-c1ccc(CN(C)C)cc1 |
Structure |
|