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Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

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Probe Reports from the NIH Molecular Libraries Program [Internet].

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Table 3SAR Analysis for Selective κ–opioid receptor agonist for the Bisamide Scaffold

SAR Analysis for KOR Selective Scaffolds (Medicinal Chemistry & Cheminformatics Analysis)
Image ml139fu11.jpg
Potency (µM) Ave. ± S.E.M. (n = replicates)

n value in column refers to KOR DRx replicates
#CIDSIDBCCG MLS-*R1R2R3XR4NKOR DRxKOR HCS (n=2)MOR HCS (n=2)DOR HCS (n=2)
15236771872187820254632PC6H11C5H10S2-pyridyl30.12 ±0.01<0.06>32>32
24014737872187830211381PC6H11C5H10S2-pyrazinyl30.44 ±0.060.14>32>32
33950926872187810075520PC6H11C5H10O2-pyridyl30.82 ±0.040.13>32>32
41282817872187980425703Pp-Br-C6H4C5H10O2-pyridyl30.42 ±0.020.10>32>32
54579040872187970079438PC5H9C5H10O2-pyrazinyl3>10>32>32>32
61297443872187670024680P2,6-dimethyl- C6H4C4H8O2-pyridyl34.05 ±0.101.11>32>32
73950572872187800237946PC5H9MeEtS2-pyridyl32.07 ±0.170.81>32>32
83242935872187960007493PC6H11MeEtO2-pyrazinyl33.71 ±0.191.36>32>32
93964693872187950080731PC6H11MeEtO2-pyridyl30.65 ±0.030.17>32>32
101458208857870730435478SC6H11HHS2-pyridyl2>20NDNDND
1144483222857870750435480SC6H11HHS3-pyridyl2>20NDNDND
1244483224857870740435479SC7H13HHS2-pyridyl2>20NDNDND
1344483221857870770435482SC7H13HHS3-pyridyl2>20NDNDND
1444483223857870760435481SMeO**HHS3-pyridyl2>20NDNDND
*

S = Synthesized P = purchased

**

methyl ester instead of methyl amide

ND = not determined

TBA = to be assigned

Bold underlined compound = probe submitted

Underlined italicized cmpd # = analog submitted

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