Reaction Details |
| Report a problem with these data |
Target | Histamine H3 receptor |
---|
Ligand | BDBM27205 |
---|
Substrate/Competitor | BDBM22530 |
---|
Meas. Tech. | Radioligand Binding Assay |
---|
pH | 7.4±n/a |
---|
Temperature | 298.15±n/a K |
---|
Ki | 23.4±n/a nM |
---|
Citation | Zhao, C; Sun, M; Bennani, YL; Gopalakrishnan, SM; Witte, DG; Miller, TR; Krueger, KM; Browman, KE; Thiffault, C; Wetter, J; Marsh, KC; Hancock, AA; Esbenshade, TA; Cowart, MD The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem51:5423-30 (2008) [PubMed] Article |
---|
More Info.: | Get all data from this article, Solution Info, Assay Method |
---|
|
Histamine H3 receptor |
---|
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: | MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
|
|
|
BDBM27205 |
---|
BDBM22530 |
---|
Name | BDBM27205 |
Synonyms: | Conessine analogue, 12k | N-methyl-N-[(1R,2S,5S,6S,9R,12S,13R,16S)-6,7,13-trimethyl-7-azapentacyclo[10.8.0.0^{2,9}.0^{5,9}.0^{13,18}]icos-18-en-16-yl]ethane-1-sulfonamide |
Type | Small organic molecule |
Emp. Form. | C25H42N2O2S |
Mol. Mass. | 434.678 |
SMILES | [H][C@@]1(C)N(C)C[C@]23CC[C@@]4([H])[C@@]([H])(CC=C5C[C@H](CC[C@]45C)N(C)S(=O)(=O)CC)[C@]2([H])CC[C@]13[H] |r,t:14| |
Structure |
|