Reaction Details Report a problem with these data
Target
Histamine H3 receptor
Ligand
BDBM50405116
Substrate
n/a
Meas. Tech.
ChEMBL_1738556 (CHEMBL4154306)
EC50
0.300±n/a nM
Citation
 Ghoshal, A; Kumar, A; Yugandhar, D; Sona, C; Kuriakose, S; Nagesh, K; Rashid, M; Singh, SK; Wahajuddin, M; Yadav, PN; Srivastava, AK Identification of novel ?-lactams and pyrrolidinone derivatives as selective Histamine-3 receptor (H3R) modulators as possible anti-obesity agents. Eur J Med Chem 152:148-159 (2018) [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:
BDBM50405116
Synonyms:
CHEMBL4177416
Type:
Small organic molecule
Emp. Form.:
C30H30F2N2O5
Mol. Mass.:
536.5664
SMILES:
COc1cc(cc(OC)c1OC)N1C(=O)\C(=C/c2ccccc2)C1(C(=O)NC(C)(C)C)c1cc(F)cc(F)c1
Structure:
Search PDB for entries with ligand similarity: