KSC-12-192
# KSC-12-192

KSC-12-192 is a drug that is used in scientific research to study the κ-opioid receptor, where it acts as a biased agonist.

KSC-12-192 preferentially activates G-protein coupling over β-arrestin 2 recruitment in vitro, an intrinsic activity shared with many other KOR ligands developed to separate KOR-mediated analgesia from accompanying dysphoria.

Compared with most of the known KOR G-protein biased agonists, KSC-12-192 and its parent compound ML138 do not exhibit stereoisomerism.

Out of a range of tested compounds with the same substituted triazole scaffold (see table), KSC-12-192 had the highest reported in vitro potency as a human KOR agonist $(EC_{50}$ = 31nM).

| Identifiers | Identifiers | X | $R_1$ | $R_2$ | $R_3$ |
| - | - | - | - | - | - |
| | KSC-12-192 | O | H | $CH_3$ | $CF_3$ |
| ML138 | KSC-5-240 | O | H | Cl | Cl |
| | KSC-12-193 | S | H | $CH_3$ | $CF_3$ |
| | KSC-5-247G | S | H | Cl | Cl |
| | KSC-12-238-B5 | O | $CH_3$ | $CH_3$ | $CF_3$ |
| | KSC-12-238-B4 | O | $CH_3$ | Cl | Cl |
