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Target
Histamine H3 receptor
Ligand
BDBM50606406
Substrate
n/a
Meas. Tech.
ChEMBL_2254798 (CHEMBL5169008)
Kd
<1000±n/a nM
Citation
 Kok, ZY; Stoddart, LA; Mistry, SJ; Mocking, TAM; Vischer, HF; Leurs, R; Hill, SJ; Mistry, SN; Kellam, B Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H J Med Chem 65:8258-8288 (2022) [PubMed] 
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:
BDBM50606406
Synonyms:
CHEMBL5184108
Type:
Small organic molecule
Emp. Form.:
C65H78BF2N11O11S
Mol. Mass.:
1270.255
SMILES:
CC(C)[C@H](NC(=O)CCN1CCC(CC1)Oc1ccccc1Cc1ccccc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)NCCC(=O)N[C@@H](CCCCNC(=O)COc1ccc(\C=C\C2=[N+]3C(C=C2)=Cc2ccc(-c4cccs4)n2[B-]3(F)F)cc1)C(N)=O |r,c:73,75,t:70|
Structure:
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