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Target
Histamine H3 receptor
Ligand
BDBM50268453
Substrate
n/a
Meas. Tech.
ChEMBL_523452 (CHEMBL1008304)
EC50
405±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:
BDBM50268453
Synonyms:
(5-(1-isopropylpiperidin-4-yloxy)-2-methyl-1H-indol-3-yl)(morpholino)methanone | CHEMBL496814
Type:
Small organic molecule
Emp. Form.:
C22H31N3O3
Mol. Mass.:
385.4998
SMILES:
CC(C)N1CCC(CC1)Oc1ccc2[nH]c(C)c(C(=O)N3CCOCC3)c2c1
Structure:
Search PDB for entries with ligand similarity: