Ki Summary

Reaction Details

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Target

KiSS-1 receptor

Ligand

BDBM50392492

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_852184 (CHEMBL2157605)

EC50

0.15±n/a nM

Citation

Asami, T; Nishizawa, N; Ishibashi, Y; Nishibori, K; Horikoshi, Y; Matsumoto, H; Ohtaki, T; Kitada, C Trypsin resistance of a decapeptide KISS1R agonist containing an N¿-methylarginine substitution. Bioorg Med Chem Lett22:6328-32 (2012) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

KiSS-1 receptor

Name:

KiSS-1 receptor

Synonyms:

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:

MHTVATSGPNASWGAPANASGCPGCGANASDGPVPSPRAVDAWLVPLFFAALMLLGLVGN
SLVIYVICRHKPMRTVTNFYIANLAATDVTFLLCCVPFTALLYPLPGWVLGDFMCKFVNY
IQQVSVQATCATLTAMSVDRWYVTVFPLRALHRRTPRLALAVSLSIWVGSAAVSAPVLAL
HRLSPGPRAYCSEAFPSRALERAFALYNLLALYLLPLLATCACYAAMLRHLGRVAVRPAP
ADSALQGQVLAERAGAVRAKVSRLVAAVVLLFAACWGPIQLFLVLQALGPAGSWHPRSYA
AYALKTWAHCMSYSNSALNPLLYAFLGSHFRQAFRRVCPCAPRRPRRPRRPGPSDPAAPH
AELLRLGSHPAPARAQKPGSSGLAARGLCVLGEDNAPL

BDBM50392492

n/a

Name

BDBM50392492

Synonyms:

CHEMBL2152062

Type

Small organic molecule

Emp. Form.

C62H81N17O14

Mol. Mass.

1288.412

SMILES

CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |r,wU:59.62,37.50,23.26,72.75,wD:51.58,29.34,12.20,4.4,82.85,(21.35,-5.83,;21.35,-4.29,;22.67,-3.52,;20.01,-3.52,;20.01,-1.98,;18.68,-1.21,;17.35,-1.98,;17.35,-3.52,;16.01,-1.21,;14.68,-1.98,;13.34,-1.21,;13.34,.33,;12.01,-1.98,;12.01,-3.52,;13.34,-4.29,;14.68,-3.52,;16.02,-4.29,;16.02,-5.83,;14.68,-6.6,;13.34,-5.83,;10.67,-1.21,;9.35,-1.98,;9.35,-3.52,;8,-1.21,;8,.33,;9.35,1.1,;6.67,-1.98,;5.34,-1.21,;5.34,.33,;4,-1.98,;4,-3.52,;5.34,-4.29,;6.67,-3.52,;5.34,-5.83,;2.67,-1.21,;1.34,-1.98,;1.34,-3.52,;-.01,-1.21,;-.01,.33,;1.34,1.1,;2.74,.48,;3.77,1.62,;3,2.96,;3.48,4.42,;2.46,5.57,;.94,5.24,;.47,3.78,;1.5,2.64,;-1.33,-1.98,;-2.67,-1.21,;-2.67,.33,;-4,-1.98,;-4,-3.52,;-2.67,-4.29,;-1.33,-3.52,;-2.67,-5.83,;-5.33,-1.21,;-6.67,-1.98,;-6.67,-3.52,;-8.01,-1.21,;-9.34,-1.98,;-8.01,.33,;-6.67,1.1,;-5.33,.33,;-4,1.1,;-4,2.64,;-2.67,3.41,;-5.33,3.41,;-6.67,2.64,;21.35,-1.21,;21.35,.33,;22.67,-1.98,;24.02,-1.21,;24.02,.34,;25.36,1.12,;25.36,2.66,;26.7,3.44,;26.71,4.99,;28.04,2.66,;25.35,-1.98,;25.35,-3.52,;26.68,-1.21,;28.02,-1.98,;28.02,-3.52,;29.35,-4.29,;30.69,-3.52,;32.03,-4.29,;32.03,-5.83,;30.68,-6.6,;29.35,-5.83,;29.35,-1.21,;30.68,-1.98,;29.35,.33,)|

Structure