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

General Information of DTT (ID: TTZN7RP)

• DTT Name: Rho-associated protein kinase 1 (ROCK1) DTT Info
• Gene Name: ROCK1

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Netarsudil	DM0LPI9	Open-angle glaucoma	9C61	Approved	[1]

4 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
H-1152	DM8XH3S	Pulmonary arterial hypertension	BB01.0	Phase 2	[2]
SAR-407899	DMF95KD	Diabetic nephropathy	GB61.Z	Phase 2	[3]
INS-117548	DMA46DO	Glaucoma/ocular hypertension	9C61	Phase 1	[4]
GSK269962A	DM5I2HL	Inflammation	1A00-CA43.1	Clinical trial	[5]

9 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID28048944-Compound-19	DMPT3V9	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-2	DM9ZXOP	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-20	DM19BQ6	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-21	DMPNG9C	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-3	DM1BN74	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-4	DMJAUWG	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-5	DMAB987	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-6	DM5RCBV	N. A.	N. A.	Patented	[6]
PMID28048944-Compound-7	DMXZ368	N. A.	N. A.	Patented	[6]

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	[7]

20 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(4-Fluoro-phenyl)-(9H-purin-6-yl)-amine	DM75EAT	Discovery agent	N.A.	Investigative	[8]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[9]
Acid-activated omeprazole	DMTOEJX	Discovery agent	N.A.	Investigative	[10]
AMA-237	DMW9TRD	Chronic obstructive pulmonary disease	CA22	Investigative	[11]
AS-1892802	DMS86PI	Pain	MG30-MG3Z	Investigative	[11]
ATS-907	DMHEK4U	Glaucoma/ocular hypertension	9C61	Investigative	[11]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[12]
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[12]
Fasudil	DMTCNOM	Discovery agent	N.A.	Investigative	[13]
KN-62	DMLZ89P	Discovery agent	N.A.	Investigative	[12]
KT-5720	DM9J50F	Discovery agent	N.A.	Investigative	[12]
PMID19364658C33	DMSE1C3	Discovery agent	N.A.	Investigative	[14]
PMID20462760C22	DMQFKBI	Discovery agent	N.A.	Investigative	[15]
PMID20684608C35	DMVUEZI	Discovery agent	N.A.	Investigative	[16]
RKI-1447	DMGTAWC	Discovery agent	N.A.	Investigative	[17]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[12]
Ro31-8220	DMDJLF0	Discovery agent	N.A.	Investigative	[12]
SB-747651A	DM20Q5O	Discovery agent	N.A.	Investigative	[18]
SR-3850	DM3Y09Z	Solid tumour/cancer	2A00-2F9Z	Investigative	[11]
TRN-101	DMXNSTF	Chronic obstructive pulmonary disease	CA22	Investigative	[11]

References

• [1] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [2] Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19.
• [3] The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. J Hypertens. 2012 May;30(5):980-9.
• [4] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [5] Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.
• [6] Rho kinase inhibitors: a patent review (2014 - 2016).Expert Opin Ther Pat. 2017 Apr;27(4):507-515.
• [7] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025959)
• [8] Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
• [9] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
• [10] Long-term treatment with a specific Rho-kinase inhibitor suppresses cardiac allograft vasculopathy in mice. Circ Res. 2004 Jan 9;94(1):46-52.
• [11] 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: 1503).
• [12] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [13] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [14] Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem. 2009 May 1;17(9):3342-51.
• [15] 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.
• [16] Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors. J Med Chem. 2010 Aug 12;53(15):5727-37.
• [17] Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm. 2012 Jun 1;3(6):699-709.
• [18] Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-o... J Med Chem. 2008 Sep 25;51(18):5663-79.