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

General Information of Drug (ID: DMP8HW1)

Drug Name

LY2157299 Drug Info

Synonyms

Galunisertib; 700874-72-2; LY2157299; LY 2157299; LY-2157299; UNII-3OKH1W5LZE; 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide; 3OKH1W5LZE; Galunisertib (LY2157299); AK-79916; 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide; 4-(2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo-[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide; 4-[2-(6-methylpyridin-2-yl)-4H,5H,6H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide

Indication

Disease Entry	ICD 11	Status	REF
Arteriosclerosis	BD40	Phase 2/3	[1]
Non-small-cell lung cancer	2C25.Y	Phase 2/3	[2]
Hepatocellular carcinoma	2C12.02	Phase 2	[2]
Glioma	2A00.0	Phase 1/2	[3]
Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[2]
Pancreatic cancer	2C10	Phase 1	[2]

Cross-matching ID

PubChem CID: 10090485
ChEBI ID: CHEBI:137064
CAS Number: CAS 700874-72-2
TTD Drug ID: DMP8HW1

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
TGF-beta receptor type I (TGFBR1)	TTP4520	TGFR1_HUMAN	Modulator	[4]
Transforming growth factor beta 1 (TGFB1)	TTR9XHZ	TGFB1_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
Transforming growth factor beta 1 (TGFB1)	DTT	TGFB1	5.844	5.859	6.44	6.172
TGF-beta receptor type I (TGFBR1)	DTT	TGFBR1	6.123	5.573	5.6	5.399

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

Arteriosclerosis

ICD Disease Classification

BD40

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Transforming growth factor beta 1 (TGFB1)	DTT	TGFB1	5.95E-09	1.68	7.81

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: 7797).
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Cardiac Safety of TGF-beta Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study. Cardiovasc Toxicol. 2015 Oct;15(4):309-23.