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

General Information of Drug (ID: DMKWCTR)

Drug Name

GS-9973 Drug Info

Synonyms

Entospletinib; 1229208-44-9; GS-9973; Entospletinib (GS-9973); gs9973; UNII-6I3O3W6O3B; 6-(1H-Indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amine; GS 9973; 6I3O3W6O3B; CHEMBL3265032; C23H21N7O; 6-(1H-Indazol-6-yl)-N-(4-(morpholin-4-yl)phenyl)imidazo(1,2-a)pyrazin-8-amine; Entospletinib [INN]; Entospletinib [USAN:INN]; 4puz; 6-(1h-Indazol-6-Yl)-N-[4-(Morpholin-4-Yl)phenyl]imidazo[1,2-A]pyrazin-8-Amine; GS-9973; Entospletinib; SCHEMBL2483776; GTPL7889; MolPort-035-395-879; HMS3653D13; EX-A1120; BCP09582; AOB87385

Indication

Disease Entry	ICD 11	Status	REF
Acute myeloid leukaemia	2A60	Phase 2	[1]
B-cell lymphoma	2A86	Phase 2	[2]
Haematological malignancy	2B33.Y	Phase 2	[1]

Cross-matching ID

PubChem CID: 59473233
CAS Number: CAS 1229208-44-9
TTD Drug ID: DMKWCTR

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tyrosine-protein kinase SYK (SYK)	TTOU65C	KSYK_HUMAN	Modulator	[3]

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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
Tyrosine-protein kinase SYK (SYK)	DTT	SYK	3.485	4.618	3.954	5.98

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

Acute myeloid leukaemia

ICD Disease Classification

2A60

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tyrosine-protein kinase SYK (SYK)	DTT	SYK	5.20E-02	-0.57	-0.67

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	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: 7889).
3	An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Apr 9;125(15):2336-43.