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Target
Histamine H3 receptor
Ligand
BDBM50159110
Substrate
n/a
Meas. Tech.
ChEMBL_2168798 (CHEMBL5053857)
Ki
0.060256±n/a nM
Citation
 Rosier, N; Grätz, L; Schihada, H; Möller, J; I?bilir, A; Humphrys, LJ; Nagl, M; Seibel, U; Lohse, MJ; Pockes, S A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H J Med Chem 64:11695-11708 (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:
BDBM50159110
Synonyms:
1-(3-(4-(piperidin-1-ylmethyl)phenoxy)propyl)piperidine | 1-(4-(3-(piperidin-1-yl)propoxy)benzyl)piperidine | 1-[3-(4-hexahydro-1-pyridinylmethylphenoxy)propyl]hexahydropyridine | 1-[4-(3-hexahydro-1-pyridinylpropoxy)benzyl]hexahydropyridine | CHEMBL129542 | JNJ-5207852
Type:
Small organic molecule
Emp. Form.:
C20H32N2O
Mol. Mass.:
316.4809
SMILES:
C(COc1ccc(CN2CCCCC2)cc1)CN1CCCCC1
Structure:
Search PDB for entries with ligand similarity: