Drug Information
| Drug General Information | |||||
|---|---|---|---|---|---|
| Drug ID |
D07YHM
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| Former ID |
DIB003109
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| Drug Name |
LY-2456302
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| Synonyms |
Opioid receptor kappa (KOR) antagonist (alcohol dependence), Eli Lilly
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| Drug Type |
Small molecular drug
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| Indication | Alcohol use disorders [ICD9: 303; ICD10:F10.2] | Phase 1 | [1] | ||
| Company |
Eli Lilly & Co
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| Structure |
|
Download2D MOL |
|||
| Formula |
C26H27FN2O2
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| Canonical SMILES |
CC1=CC(=CC(=C1)C2CCCN2CC3=CC=C(C=C3)OC4=C(C=C(C=C4)C(=O<br />)N)F)C
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| InChI |
1S/C26H27FN2O2/c1-17-12-18(2)14-21(13-17)24-4-3-11-29(24)16-19-5-8-22(9-6-19)31-25-10-7-20(26(28)30)15-23(25)27/h5-10,12-15,24H,3-4,11,16H2,1-2H3,(H2,28,30)/t24-/m0/s1
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| InChIKey |
ZHPMYDSXGRRERG-DEOSSOPVSA-N
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| PubChem Compound ID | |||||
| PubChem Substance ID | |||||
| Target and Pathway | |||||
| Target(s) | Kappa-type opioid receptor | Target Info | Antagonist | [2] | |
| KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
| PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | ||||
| Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
| Opioid prodynorphin pathway | |||||
| Reactome | Peptide ligand-binding receptors | ||||
| G alpha (i) signalling events | |||||
| WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
| Peptide GPCRs | |||||
| GPCR ligand binding | |||||
| GPCR downstream signaling | |||||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT02218775) FASTMAS (New Experimental Medicine Studies: Fast-Fail Trials in Mood and Anxiety Spectrum Disorders) Kappa Opioid Receptor (KOR) Phase 1 Study. U.S. National Institutes of Health. | ||||
| REF 2 | LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44. | ||||
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