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

General Information of Drug (ID: DM457B1)

Drug Name

FK-888 Drug Info

Synonyms

FK 888; FK-888; 138449-07-7; FK888; N(2)-(4-Hydroxy-1-(1-methyl-1H-indol-3-yl)carbonyl-L-prolyl)-N-methyl-N-phenylmethyl-3-(2-naphthyl)-L-alaninamide; SCHEMBL8079679; GTPL2114; AC1L332N; CHEMBL1416993; CHEBI:93463; DTXSID70160680; MolPort-023-276-412; HMS3269A13; ZINC3926844; PDSP2_000648; AKOS024457076; NCGC00159560-01; L-Alaninamide, trans-4-hydroxy-1-((1-methyl-1H-indol-3-yl)carbonyl)-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-; LS-193299; BRD-K83508485-001-01-9

Indication

Disease Entry	ICD 11	Status	REF
Migraine	8A80	Discontinued in Phase 2	[1]

Cross-matching ID

PubChem CID: 107967
ChEBI ID: CHEBI:93463
CAS Number: CAS 138449-07-7
TTD Drug ID: DM457B1

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[2]

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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
Substance-P receptor (TACR1)	DTT	TACR1	3.597	4.186	4.271	5.113

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

Migraine

ICD Disease Classification

8A80

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Substance-P receptor (TACR1)	DTT	TACR1	7.40E-01	0.02	0.07
Substance-P receptor (TACR1)	DTT	TACR1	8.57E-01	-0.02	-0.18

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: 2114).
2	Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist, FK888. Br J Pharmacol. 1992 Nov;107(3):785-9.