Synonyms: BTRX-246040 [1] | compound 36 [PMID: 24678969] | LY-2940094
Compound class:
Synthetic organic
Comment: LY2940094 is a potent and selective nociceptin receptor antagonist [4], with potential clinical utility as a treatment for neurobehavioral disorders [3,6].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Ferrari F, Rizzo S, Ruzza C, Calo G. (2020)
Detailed In Vitro Pharmacological Characterization of the Clinically Viable Nociceptin/Orphanin FQ Peptide Receptor Antagonist BTRX-246040. J Pharmacol Exp Ther, 373 (1): 34-43. [PMID:31937563] |
2. Post A, Smart TS, Jackson K, Mann J, Mohs R, Rorick-Kehn L, Statnick M, Anton R, O'Malley SS, Wong CJ. (2016)
Proof-of-Concept Study to Assess the Nociceptin Receptor Antagonist LY2940094 as a New Treatment for Alcohol Dependence. Alcohol Clin Exp Res, 40 (9): 1935-44. [PMID:27435979] |
3. Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M et al.. (2016)
A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies. Neuropsychopharmacology, 41 (7): 1803-12. [PMID:26585287] |
4. Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM et al.. (2014)
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold. J Med Chem, 57 (8): 3418-29. [PMID:24678969] |
5. Witkin JM, Rorick-Kehn LM, Benvenga MJ, Adams BL, Gleason SD, Knitowski KM, Li X, Chaney S, Falcone JF, Smith JW et al.. (2016)
Preclinical findings predicting efficacy and side-effect profile of LY2940094, an antagonist of nociceptin receptors. Pharmacol Res Perspect, 4 (6): e00275. [PMID:28097008] |
6. Witkin JM, Wallace TL, Martin WJ. (2019)
Therapeutic Approaches for NOP Receptor Antagonists in Neurobehavioral Disorders: Clinical Studies in Major Depressive Disorder and Alcohol Use Disorder with BTRX-246040 (LY2940094). Handb Exp Pharmacol, 254: 399-415. [PMID:30701317] |