General Information of Drug (ID: DMBJUEM)

Drug Name
ENDOMORPHIN-1 Drug Info
Synonyms
Endomorphin 1; Endomorphin-1; 189388-22-5; Tyr-Pro-Trp-Phe-Nh2; H-Tyr-Pro-Trp-Phe-NH2; CHEMBL316446; L-Phenylalaninamide,L-tyrosyl-L-prolyl-L-tryptophyl-; (S)-N-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)-1-((S)-2-amino-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide; (2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5311080
CAS Number
CAS 189388-22-5
TTD Drug ID
DMBJUEM

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Opioid receptor delta (OPRD1) TT27RFC OPRD_HUMAN Inhibitor [2]
Opioid receptor kappa (OPRK1) TTQW87Y OPRK_HUMAN Inhibitor [3]
Opioid receptor mu (MOP) TTKWM86 OPRM_HUMAN Inhibitor [4]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Opioid receptor kappa (OPRK1) DTT OPRK1 5.533 5.372 5.703 5.632
Opioid receptor mu (MOP) DTT OPRM1 4.548 5.062 4.652 4.776
Opioid receptor delta (OPRD1) DTT OPRD1 2.848 2.263 1.536 2
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Discovery agent
ICD Disease Classification N.A.
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Opioid receptor mu (MOP) DTT OPRM1 5.94E-01 -0.02 -0.17
Opioid receptor delta (OPRD1) DTT OPRD1 5.52E-01 0.03 0.23
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1623).
2 New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile. J Med Chem. 2008 Jul 24;51(14):4270-9.
3 Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. J Med Chem. 2004 Jan 29;47(3):735-43.
4 Synthesis and evaluation of new endomorphin analogues modified at the Pro(2) residue. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4115-8.