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

General Information of DTT (ID: TTWTSCV)

• DTT Name: RAC-alpha serine/threonine-protein kinase (AKT1) DTT Info
• Gene Name: AKT1

Molecule-Related Drug & Molecule List

1 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Capivasertib	DM9SKW8	Breast cancer	2C60-2C65	Approved	[1]

12 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[1]
GDC-0068	DMWBZJD	Breast cancer	2C60-2C65	Phase 3	[1]
ARQ 092	DM5WK0J	Proteus syndrome	LD2C	Phase 2	[2]
CI-1033	DMSI8N3	Lymphoma	2A80-2A86	Phase 2	[3]
CMX-2043	DMPSCVY	Cardiac disease	BA00-BE2Z	Phase 2	[4]
GSK2110183	DMZHB37	leukaemia	2A60-2B33	Phase 2	[5]
PTX-200	DM0ZIT2	Breast cancer	2C60-2C65	Phase 2	[1]
RX-0201	DMTBAV3	Pancreatic cancer	2C10	Phase 2	[6]
Triciribine prodrug	DMBN1XS	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[5]
ARQ 751	DM7MWX0	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]
BMS-754807	DMPK32V	N. A.	N. A.	Phase 1	[7]
M2698	DM3PVBJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

1 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID28460551-Compound-6	DMT7U1O	N. A.	N. A.	Patented	[8]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Squalestatin 1	DM4JZPT	Arteriosclerosis	BD40	Terminated	[9]

24 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one	DM27WDP	Discovery agent	N.A.	Investigative	[10]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[11]
4,5,6-trihydroxy-3-methylphthalide	DMQFTJ7	Discovery agent	N.A.	Investigative	[12]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[13]
A-443654	DMLMU63	Discovery agent	N.A.	Investigative	[14]
A-674563	DMJ83LK	Discovery agent	N.A.	Investigative	[15]
Akt inhibitor VIII	DMDVIT1	Discovery agent	N.A.	Investigative	[16]
ALM-301	DMY1OG7	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[17]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[18]
BX-517	DMBQIEF	Discovery agent	N.A.	Investigative	[10]
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[17]
Inositol 1,3,4,5-Tetrakisphosphate	DMIFD35	Discovery agent	N.A.	Investigative	[19]
KN-62	DMLZ89P	Discovery agent	N.A.	Investigative	[17]
Lactoquinomycin	DMZ0O1X	Haematological malignancy	2B33.Y	Investigative	[20]
LD-101	DMD5GO0	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]
MYRIOCIN	DMVXW4L	Discovery agent	N.A.	Investigative	[9]
NU-1001-41	DMEHMOK	Solid tumour/cancer	2A00-2F9Z	Investigative	[5]
PMID20005102C1	DMMESBW	Discovery agent	N.A.	Investigative	[21]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[17]
Ro31-8220	DMDJLF0	Discovery agent	N.A.	Investigative	[17]
SB-747651A	DM20Q5O	Discovery agent	N.A.	Investigative	[22]
STAUROSPORINONE	DMU2H4K	Discovery agent	N.A.	Investigative	[17]
VLI-27	DM95KRY	Pancreatic cancer	2C10	Investigative	[5]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] 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.
• [4] Pre-clinical and Clinical Safety Studies of CMX-2043: a cytoprotective lipoic acid analogue for ischaemia-reperfusion injury. Basic Clin Pharmacol Toxicol. 2014 Nov;115(5):456-64.
• [5] 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: 1479).
• [6] CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
• [7] Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in cli... J Med Chem. 2009 Dec 10;52(23):7360-3.
• [8] Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jul;27(7):753-761.
• [9] Raft nanodomains contribute to Akt/PKB plasma membrane recruitment and activation. Nat Chem Biol. 2008 Sep;4(9):538-47.
• [10] Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8.
• [11] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
• [12] A phthalide with in vitro growth inhibitory activity from an oidiodendron strain. J Nat Prod. 2004 Dec;67(12):2086-9.
• [13] 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
• [14] Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem. 2007 Jun 28;50(13):2990-3003.
• [15] Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.
• [16] Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.
• [17] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [18] Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
• [19] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [20] The PI3K/Akt pathway as a target in the treatment of hematologic malignancies. Anticancer Agents Med Chem. 2009 Jun;9(5):550-9.
• [21] 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83.
• [22] 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.