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Target
Histamine H3 receptor
Ligand
BDBM50193199
Substrate
n/a
Meas. Tech.
ChEMBL_523447 (CHEMBL1008299)
Ki
7±n/a nM
Citation
 Pierson, PD; Fettes, A; Freichel, C; Gatti-McArthur, S; Hertel, C; Huwyler, J; Mohr, P; Nakagawa, T; Nettekoven, M; Plancher, JM; Raab, S; Richter, H; Roche, O; Rodríguez Sarmiento, RM; Schmitt, M; Schuler, F; Takahashi, T; Taylor, S; Ullmer, C; Wiegand, R 5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity. J Med Chem 52:3855-68 (2009) [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:
BDBM50193199
Synonyms:
(S)-1-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)-3-(4-(trifluoromethyl)phenyl)prop-2-en-1-one | (S,E)-1-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)-3-(4-(trifluoromethyl)phenyl)prop-2-en-1-one | CHEMBL218790
Type:
Small organic molecule
Emp. Form.:
C19H23F3N2O
Mol. Mass.:
352.3939
SMILES:
FC(F)(F)c1ccc(\C=C\C(=O)N2CCC[C@H]2CN2CCCC2)cc1 |r|
Structure:
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