Target
Histamine H3 receptor
Ligand
BDBM50319508
Substrate
n/a
Meas. Tech.
ChEMBL_766669 (CHEMBL1827363)
Ki
0.2±n/a nM
Citation
 Levoin, NLabeeuw, OCalmels, TPoupardin-Olivier, OBerrebi-Bertrand, ILecomte, JMSchwartz, JCCapet, M Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity. Bioorg Med Chem Lett 21:5378-83 (2011) [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:
BDBM50319508
Synonyms:
(R)-2,4-dimethyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazole | CHEMBL1084559
Type:
Small organic molecule
Emp. Form.:
C21H25N3S
Mol. Mass.:
351.508
SMILES:
C[C@@H]1CCCN1CCc1ccc2nc(ccc2c1)-c1sc(C)nc1C |r|
Structure:
Search PDB for entries with ligand similarity: