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Target
KiSS-1 receptor
Ligand
BDBM50322306
Substrate
n/a
Meas. Tech.
ChEMBL_642624 (CHEMBL1176639)
IC50
20±n/a nM
Citation
 Kobayashi, T; Sasaki, S; Tomita, N; Fukui, S; Nakayama, M; Kiba, A; Kusaka, M; Matsumoto, S; Yamaguchi, M; Itoh, F; Baba, A 2-acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats. Bioorg Med Chem 18:5157-71 (2010) [PubMed]  Article 
Target
Name:
KiSS-1 receptor
Synonyms:
AXOR12 | G-protein Coupled Receptor 54 | G-protein coupled receptor 54 (GPR54) | GPR54 | Hypogonadotropin-1 | KISS1R | KISSR_HUMAN | KiSS-1R | Kisspeptins receptor | Metastin receptor | hOT7T175
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
42613.79
Organism:
Homo sapiens (Human)
Description:
Binding assay was performed using membranes from the CHO cell transfectants.
Residue:
398
Sequence:
MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGNSLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNYIQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLALHRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAPADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYAAYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPHAELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL
  
Inhibitor
Name:
BDBM50322306
Synonyms:
CHEMBL1173512 | N-[3-Cyano-4-{3-[(4-ethylpiperazin-1-yl)methyl]phenyl}-6-(4-fluoro-2-hydroxyphenyl)pyridin-2-yl]furan-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C30H28FN5O3
Mol. Mass.:
525.5734
SMILES:
CCN1CCN(Cc2cccc(c2)-c2cc(nc(NC(=O)c3ccco3)c2C#N)-c2ccc(F)cc2O)CC1
Structure:
Search PDB for entries with ligand similarity: