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

General Information of Drug (ID: DMGYBZI)

Drug Name

PHA-739358 Drug Info

Synonyms

Danusertib; PHA 739358; Danusertib, PHA-739358; (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide; 5-Amido-pyrrolopyrazole 9d

Indication

Disease Entry	ICD 11	Status	REF
Prostate cancer	2C82.0	Phase 2	[1]

Cross-matching ID

PubChem CID: 11442891
ChEBI ID: CHEBI:94490
CAS Number: CAS 827318-97-8
TTD Drug ID: DMGYBZI

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aurora B messenger RNA (AURKB mRNA)	TT9RTBL	AURKB_HUMAN	Inhibitor	[2]
Aurora kinase A (AURKA)	TTPS3C0	AURKA_HUMAN	Inhibitor	[3]
Aurora kinase B (AURKB)	TT5LS6T	AURKB_HUMAN	Inhibitor	[3]
Aurora kinase C (AURKC)	TTLYXIT	AURKC_HUMAN	Inhibitor	[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
Aurora kinase A (AURKA)	DTT	AURKA	4.479	5.036	4.392	4.505
Aurora B messenger RNA (AURKB mRNA)	DTT	AURKB	2.104	2.536	1.766	5.423
Aurora kinase B (AURKB)	DTT	AURKB	2.104	2.536	1.766	5.423

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

Prostate cancer

ICD Disease Classification

2C82.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Aurora kinase A (AURKA)	DTT	AURKA	9.41E-46	-1.78	-2.05
Aurora kinase B (AURKB)	DTT	AURKB	3.52E-36	-0.82	-1.62

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: 7937).
2	Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem. 2005 Apr 21;48(8):3080-4.
3	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.