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Target
Histamine H3 receptor
Ligand
BDBM50146835
Substrate
n/a
Meas. Tech.
ChEMBL_2079146 (CHEMBL4734937)
Ki
1.2±n/a nM
Citation
 Szczepa?ska, K; Pockes, S; Podlewska, S; Höring, C; Mika, K; Latacz, G; Bednarski, M; Siwek, A; Karcz, T; Nagl, M; Bresinsky, M; Mönnich, D; Seibel, U; Kuder, KJ; Kota?ska, M; Stark, H; Elz, S; Kie?-Kononowicz, K Structural modifications in the distal, regulatory region of histamine H Eur J Med Chem 213:0 (2021) [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:
BDBM50146835
Synonyms:
1-(4-Chloro-phenyl)-4-(4-cyclopentyl-piperazin-1-yl)-butane-1,4-dione; hydrochloride | CHEMBL97170
Type:
Small organic molecule
Emp. Form.:
C19H25ClN2O2
Mol. Mass.:
348.867
SMILES:
Clc1ccc(cc1)C(=O)CCC(=O)N1CCN(CC1)C1CCCC1
Structure:
Search PDB for entries with ligand similarity: