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

General Information of Drug (ID: DM0SCK8)

• Drug Name: Glycyl-H 1152 Drug Info
• Synonyms: glycyl-H 1152

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 11976582
  TTD Drug ID: DM0SCK8

Molecule-Related Drug Atlas

Drug(s) Targeting Rho-associated protein kinase 2 (ROCK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Belumosudil	DM548TK	Graft-versus-host disease	4B24	Approved	[2]
INS-117548	DMA46DO	Glaucoma/ocular hypertension	9C61	Phase 1	[3]
GSK269962A	DM5I2HL	Inflammation	1A00-CA43.1	Clinical trial	[4]
PMID28048944-Compound-19	DMPT3V9	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-3	DM1BN74	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-7	DMXZ368	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-4	DMJAUWG	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-5	DMAB987	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-6	DM5RCBV	N. A.	N. A.	Patented	[5]
PMID28048944-Compound-2	DM9ZXOP	N. A.	N. A.	Patented	[5]

Drug(s) Targeting Aurora kinase C (AURKC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PHA-739358	DMGYBZI	Prostate cancer	2C82.0	Phase 2	[6]
ABT-348	DMMZOYN	Haematological malignancy	2B33.Y	Phase 2	[7]
HPP-607	DM5VSZR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
AMG 900	DMASGXJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
SNS-314	DMAC5F2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
GSK1070916	DMXRPT6	Advanced solid tumour	2A00-2F9Z	Phase 1	[11]
GSK1070916A	DMCJUI9	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
MK-6592	DMB5NOI	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 1	[12]
Indirubin-3'-monoxime	DMLRQH0	Discovery agent	N.A.	Investigative	[13]
SU 6656	DMF1P6W	Discovery agent	N.A.	Investigative	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Aurora kinase C (AURKC)	TTLYXIT	AURKC_HUMAN	Inhibitor	[1]
Rho-associated protein kinase 2 (ROCK2)	TTGWKQJ	ROCK2_HUMAN	Inhibitor	[1]

References

• [1] Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52.
• [2] Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism. Proc Natl Acad Sci U S A. 2014 Nov 25;111(47):16814-9.
• [3] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [4] Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.
• [5] Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.
• [6] 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.
• [7] Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
• [8] 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: 1936).
• [9] Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
• [10] SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
• [11] Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
• [12] Clinical experience with aurora kinase inhibitors: a review. Oncologist. 2009 Aug;14(8):780-93.
• [13] An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted in... J Med Chem. 2007 Aug 23;50(17):4027-37.
• [14] The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.