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Target
Histamine H3 receptor
Ligand
BDBM22914
Substrate
n/a
Meas. Tech.
ChEMBL_1973743 (CHEMBL4606561)
IC50
20±n/a nM
Citation
 Bartole, E; Grätz, L; Littmann, T; Wifling, D; Seibel, U; Buschauer, A; Bernhardt, G UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H J Med Chem 63:5297-5311 (2020) [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:
BDBM22914
Synonyms:
CHEMBL260374 | N-cyclohexyl-4-(1H-imidazol-5-yl)piperidine-1-carbothioamide | Thioperamide | US11622967, Compound Thioperamide
Type:
Small organic molecule
Emp. Form.:
C15H24N4S
Mol. Mass.:
292.443
SMILES:
S=C(NC1CCCCC1)N1CCC(CC1)c1cnc[nH]1
Structure:
Search PDB for entries with ligand similarity: