Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM2V7U1)

Drug Name

FR-181157 Drug Info

Synonyms

SCHEMBL7960020; GTPL5854; FR181157; FR 181157; 2-[3-[[2-[4,5-di(phenyl)-1,3-oxazol-2-yl]-1-cyclohex-2-enyl]methyl]phenoxy]acetic acid

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

Cross-matching ID

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Prostacyclin receptor (PTGIR)	TTOFYT1	PI2R_HUMAN	Inhibitor	[2]
Prostaglandin E2 receptor EP3 (PTGER3)	TTPNGDE	PE2R3_HUMAN	Inhibitor	[3]
Prostaglandin E2 receptor EP4 (PTGER4)	TT79WV3	PE2R4_HUMAN	Inhibitor	[4]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Prostaglandin E2 receptor EP3 (PTGER3)	DTT	PTGER3	4.768	4.711	6.12	3.579
Prostacyclin receptor (PTGIR)	DTT	PTGIR	6.384	3.7	4.684	4.603
Prostaglandin E2 receptor EP4 (PTGER4)	DTT	PTGER4	4.907	7.298	6.097	7.251

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
Prostaglandin E2 receptor EP4 (PTGER4)	DTT	PTGER4	5.27E-01	-0.05	-0.1

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: 5854).
2	Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4861-4.
3	Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3284-7.
4	Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists. J Med Chem. 2005 May 5;48(9):3103-6.