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

General Information of Drug (ID: DMYDTJ6)

Drug Name

CEP-11981 Drug Info

Synonyms

CEP-11981; UNII-J8AY0Z4CBP; 856691-93-5; J8AY0Z4CBP; CHEMBL2010872; BOL-303213X; compound 11b [PMID 22148921]; GTPL8189; SCHEMBL2439310; DTXSID80234942; CEP11981; BDBM50379186; CEP 11981; 4H-Indazolo(5,4-a)pyrrolo(3,4-C)carbazol-4-one, 2,5,6,11,12,13-hexahydro-2-methyl-11-(2-methylpropyl)-8-(2-pyrimidinylamino)-; Z-3152

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1] , [2]

Cross-matching ID

PubChem CID: 11751922
CAS Number: CAS 856691-93-5
TTD Drug ID: DMYDTJ6

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiopoietin 1 receptor (TEK)	TT9VGXW	TIE2_HUMAN	Modulator	[3]
Vascular endothelial growth factor receptor 1 (FLT-1)	TT2Q6G1	VGFR1_HUMAN	Modulator	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_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
Angiopoietin 1 receptor (TEK)	DTT	TEK	5.194	5.051	6.613	4.982
Vascular endothelial growth factor receptor 1 (FLT-1)	DTT	FLT1	4.802	4.95	4.597	3.17

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

Solid tumour/cancer

ICD Disease Classification

2A00-2F9Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Vascular endothelial growth factor receptor 2 (KDR)	DTT	KDR	1.98E-01	0.11	0.2

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: 8189).
2	ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health.
3	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. (Target id: 1842).
4	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.