Target
Histamine H3 receptor
Ligand
BDBM50514107
Substrate
n/a
Meas. Tech.
ChEMBL_1855646 (CHEMBL4356375)
EC50
0.630957±n/a nM
Citation
 Wágner, GMocking, TAMArimont, MProvensi, GRani, BSilva-Marques, BLatacz, GDa Costa Pereira, DKaratzidou, CVischer, HFWijtmans, MKie?-Kononowicz, Kde Esch, IJPLeurs, R 4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H J Med Chem 62:10848-10866 (2019) [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:
BDBM50514107
Synonyms:
CHEMBL4535316
Type:
Small organic molecule
Emp. Form.:
C13H19N5O4
Mol. Mass.:
309.3211
SMILES:
OC(=O)\C=C\C(O)=O.CCNC1CN(C1)c1ccnc(N)n1
Structure:
Search PDB for entries with ligand similarity: