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Target
Histamine H3 receptor
Ligand
BDBM438124
Substrate
n/a
Meas. Tech.
[35S]-GTPgamma-delta binding assay (antagonist)
IC50
>1000±n/a nM
Citation
 Xiang, J; Xu, X; Feng, Y; Eng, W Compounds as neuronal histamine receptor-3 antagonists and uses thereof US Patent  US10618886 Publication Date 4/14/2020 
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:
BDBM438124
Synonyms:
US10618886, Compound XIX | US10730853, Compound XIX | US11420955, Compound XIX
Type:
Small organic molecule
Emp. Form.:
C27H30F5N3O3S
Mol. Mass.:
571.602
SMILES:
Cc1nc2ccc(cc2c(=O)n1-c1ccc(OC2CCN(CC2)C(=O)C2CCCCC2)cc1)S(F)(F)(F)(F)F
Structure:
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