Target
KiSS-1 receptor
Ligand
BDBM26340
Substrate
[125I]Kisspeptin-15
Meas. Tech.
Receptor Binding Assay
pH
7.3±n/a
Temperature
298.15±n/a K
IC50
1.2±n/a nM
Citation
 Tomita, KOishi, SOhno, HPeiper, SCFujii, N Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase. J Med Chem 51:7645-9 (2008) [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:
BDBM26340
Synonyms:
(2S)-N-[(1S)-4-carbamimidamido-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}butyl]-2-{3-[(2S)-2-[(4-fluorophenyl)formamido]-3-phenylpropanamido]propyl}-4-methylpentanamide | Peptide analogue, 20
Type:
n/a
Emp. Form.:
C42H54FN9O5
Mol. Mass.:
783.9339
SMILES:
CC(C)C[C@H](CCCNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O |r,wU:32.33,wD:11.19,4.4,43.44,(10.76,-1.42,;10.76,.12,;12.1,.89,;9.43,.89,;9.43,2.43,;8.09,3.2,;6.76,2.43,;5.43,3.2,;4.09,2.43,;2.76,3.2,;2.76,4.74,;1.43,2.43,;1.43,.89,;.66,-.45,;-.87,-.66,;-1.45,-2.09,;-.5,-3.3,;1.02,-3.09,;1.6,-1.66,;.09,3.2,;-1.24,2.43,;-1.24,.89,;-2.57,3.2,;-2.57,4.74,;-3.91,5.51,;-5.24,4.74,;-6.58,5.51,;-5.24,3.2,;-3.91,2.43,;10.76,3.2,;10.76,4.74,;12.1,2.43,;13.43,3.2,;13.43,4.74,;12.1,5.51,;12.1,7.05,;10.76,7.82,;10.76,9.36,;12.1,10.13,;9.43,10.13,;14.76,2.43,;14.76,.89,;16.1,3.2,;17.43,2.43,;17.43,.89,;18.76,.12,;18.15,-1.3,;19.3,-2.32,;20.63,-1.53,;22.1,-2,;23.23,-.96,;22.9,.55,;21.43,1.01,;20.3,-.03,;18.76,3.2,;20.1,2.43,;18.76,4.74,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
[125I]Kisspeptin-15
Synonyms:
n/a
Type:
radiolabeled peptide
Mol. Mass.:
1872.07
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
KDLPNYNWNSFGLRF