KISS1-305 | Agonist of KISS1R
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KISS1R
  • Ki:0.089 nM
  • Ki:0.10 nM
  • IC50:8.94 nM
Agonist
10-1000 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Binding against NPFFR2 (GPR74) and NPFFR1 (GPR147) >30 fold Clean GPCR scan with the exception for O ...

Potency
Cellular
In Vitro

KISS1R

Mode of Action: Agonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm401056w

In Vivo Validations

Rat
Dose: 30 nM/kg
Route of delivery: Subcutaneous

DOI Reference: 10.1021/jm401056w

Negative Control Compounds

KISS1-543
Notes: EC50 > 10 µM agonist activity for hKISS1R (C-terminal ethyl amide)

Chemical Information

Molecular Formula C56H76N16O12
SMILEs CNC(=N)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)NNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](Cc1ccncc1)NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
InChI InChI=1S/C56H76N16O12/c1-32(2)25-41(50(79)64-39(15-10-22-63-55(60)61-3)49(78)65-40(47(59)76)27-33-11-6-4-7-12-33)70-56(84)72-71-54(83)43(28-34-13-8-5-9-14-34)67-53(82)45(31-73)69-52(81)44(30-46(58)75)68-51(80)42(29-36-20-23-62-24-21-36)66-48(77)38(57)26-35-16-18-37(74)19-17-35/h4-9,11-14,16-21,23-24,32,38-45,73-74H,10,15,22,25-31,57H2,1-3H3,(H2,58,75)(H2,59,76)(H,64,79)(H,65,78)(H,66,77)(H,67,82)(H,68,80)(H,69,81)(H,71,83)(H3,60,61,63)(H2,70,72,84)/t38-,39+,40+,41+,42-,43+,44+,45+/m1/s1
Molecular weight 1164.58 Da
AlogP -3.0840300000000225
HBond acceptors 28
HBond donors 20
Atoms 160

Expert Reviews


No SERP comments found for KISS1-305

Probe KISS1-305 is in the process of SERP review.

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