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

General Information of DTT (ID: TTGWKQJ)

• DTT Name: Rho-associated protein kinase 2 (ROCK2) DTT Info
• Gene Name: ROCK2

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Belumosudil	DM548TK	Graft-versus-host disease	4B24	Approved	[1]

2 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INS-117548	DMA46DO	Glaucoma/ocular hypertension	9C61	Phase 1	[2]
GSK269962A	DM5I2HL	Inflammation	1A00-CA43.1	Clinical trial	[3]

13 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Indazolyl-thiadiazolamine derivative 1	DMR2GW1	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-11	DMQ6WEN	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-19	DMPT3V9	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-2	DM9ZXOP	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-3	DM1BN74	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-4	DMJAUWG	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-5	DMAB987	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-6	DM5RCBV	N. A.	N. A.	Patented	[4]
PMID28048944-Compound-7	DMXZ368	N. A.	N. A.	Patented	[4]
Tricyclic compound 4	DMEIG16	N. A.	N. A.	Patented	[4]
Tricyclic compound 5	DMLPMS7	N. A.	N. A.	Patented	[4]
Tricyclic compound 6	DMMJ81G	N. A.	N. A.	Patented	[4]
Tricyclic compound 7	DME84S5	N. A.	N. A.	Patented	[4]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CDE-5110	DMGQ9WP	Inflammation	1A00-CA43.1	Terminated	[5]

9 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMA-237	DMW9TRD	Chronic obstructive pulmonary disease	CA22	Investigative	[6]
ATS-907	DMHEK4U	Glaucoma/ocular hypertension	9C61	Investigative	[6]
Glycyl-H 1152	DM0SCK8	Discovery agent	N.A.	Investigative	[7]
PMID20462760C22	DMQFKBI	Discovery agent	N.A.	Investigative	[8]
PMID20471253C32	DMBQAKO	Discovery agent	N.A.	Investigative	[9]
PMID20684608C35	DMVUEZI	Discovery agent	N.A.	Investigative	[10]
RKI-1447	DMGTAWC	Discovery agent	N.A.	Investigative	[11]
SR-3850	DM3Y09Z	Solid tumour/cancer	2A00-2F9Z	Investigative	[6]
TRN-101	DMXNSTF	Chronic obstructive pulmonary disease	CA22	Investigative	[6]

References

• [1] 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.
• [2] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [3] Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.
• [4] Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.
• [5] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025959)
• [6] 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: 1504).
• [7] Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52.
• [8] Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3235-9.
• [9] Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3746-9.
• [10] Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors. J Med Chem. 2010 Aug 12;53(15):5727-37.
• [11] Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun 1;3(6):699-709.