Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM27208
Substrate
BDBM22530
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
298.15±n/a K
Ki
0.22±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 Chem 51:5423-30 (2008) [PubMed] Article
More Info.:
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:
Human
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
Inhibitor
Name:
BDBM27208
Synonyms:
(2S,3S)-2-amino-N,3-dimethyl-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]pentanamide | Conessine analogue, 13a
Type:
Small organic molecule
Emp. Form.:
C29H49N3O
Mol. Mass.:
455.7189
SMILES:
[H][C@@]1(C)N(C)C[C@]23CC[C@@]4([H])[C@@]([H])(CC=C5C[C@H](CC[C@]45C)N(C)C(=O)[C@@H](N)[C@@H](C)CC)[C@]2([H])CC[C@]13[H] |r,t:14|