Table 9Comparison of prior art and current probe

Antagonist NameJDTic (11)NorBNI – Norbinaltorphimine (12,13)BNI – Binaltorphimine (13,14)GNTI – Guanidinyl- naltrindole di-trifluoroacetate (15)Current 2nd Probe
ML190 (IC50 not Ki)
Prior 1st Probe
ML140 (IC50 not Ki)
Chemical Structure
Image ml190fu2.jpg
Image ml190fu3.jpg
Image ml190fu4.jpg
Image ml190fu5.jpg
Image ml190t9f1.jpg
Image ml190t9f2.jpg
Ki KOR (nM) nM (IC50 DiscoveRx)
3.0 (IC50 HCS)
850 (IC50 DiscoveRx)
1310 (IC50 DiscoveRx)
Ki MOR (nM)2.1 (202X)16.7 (417X)1.26 (9X)36.9 (923X)>32,000 (>10,700X)>32,000 (>25X)
Ki DOR (nM)300 (15,000X)10.2 (255X)5.81 (42X)70 (17500X)>32,000 (>10,700X)>32,000 (>25X)
PubChem CID9956146548023054841979853099446656803342390
PubChem SIDs:46052753; 24225384; 1493178750104378; 49963059; 47959969; 47810970; 26751686; 14937121; 14912769; 11693572; 7980165; 84186524600619; 51940254; 14863933; 66963114815182; 17405121; 50106355; 53777665; 242784548844299787218794
PMID114955799857089283966410822054Not applicable

From: Antagonist for the Kappa Opioid Receptor

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

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