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

General Information of DTT (ID: TT4TQBX)

• DTT Name: Extracellular signal-regulated kinase 2 (ERK2) DTT Info
• UniProt ID: MK01_HUMAN
• Gene Name: MAPK1

Molecule-Related Drug & Molecule List

7 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BVD-523	DMNB4XK	Melanoma	2C30	Phase 2	[1]
ASTX029	DMVZXIA	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[2]
HH2710	DM0C5MV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[3]
GDC-0994	DMFC2OY	Solid tumour/cancer	2A00-2F9Z	Phase 1	[4]
JSI-1187	DMVJWBS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
LY3214996	DMFDAY7	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
VAN-10-4-eluting stent	DM3ZW6A	Artery stenosis	BD52	Phase 1	[7]

1 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CHIR-99021	DMB8MNU	Allergic inflammation	4A80-4A85	Patented	[8]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
COR-D	DMLXMCB	T-cell leukaemia	2A90	Preclinical	[9]

1 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SB220025	DMSBUET	Arthritis	FA20	Terminated	[10]

17 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(4-Fluoro-phenyl)-(9-methyl-9H-purin-6-yl)-amine	DMYAJQU	Discovery agent	N.A.	Investigative	[11]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole	DMN9YOB	Discovery agent	N.A.	Investigative	[12]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[13]
AEZS-131	DMN9RE5	Solid tumour/cancer	2A00-2F9Z	Investigative	[14]
Bisindolylmaleimide-I	DMOQJZC	Discovery agent	N.A.	Investigative	[15]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[16]
CI-1040	DMF3DZX	Discovery agent	N.A.	Investigative	[15]
DEBROMOHYMENIALDISINE	DMDLER8	Discovery agent	N.A.	Investigative	[17]
ERK inhibitor III	DMB3ROZ	Discovery agent	N.A.	Investigative	[18]
FR-180204	DM051PI	Discovery agent	N.A.	Investigative	[19]
KN-62	DMLZ89P	Discovery agent	N.A.	Investigative	[15]
KT-5720	DM9J50F	Discovery agent	N.A.	Investigative	[15]
Phosphonothreonine	DMTFHPI	Discovery agent	N.A.	Investigative	[10]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[15]
Ro-4396686	DM5DMCH	Discovery agent	N.A.	Investigative	[20]
Ro31-8220	DMDJLF0	Discovery agent	N.A.	Investigative	[15]
SCH772984	DMWVH62	Discovery agent	N.A.	Investigative	[21]

References

• [1] DOI: 10.1158/1538-7445.AM2015-4693
• [2] Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
• [3] Clinical pipeline report, company report or official report of HaiHe Biopharma.
• [4] ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
• [5] National Cancer Institute Drug Dictionary (drug name JSI1187).
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
• [8] Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
• [9] Corchorusin-D directed apoptosis of K562 cells occurs through activation of mitochondrial and death receptor pathways and suppression of AKT/PKB pathway. Cell Physiol Biochem. 2012;30(4):915-26.
• [10] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [11] Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
• [12] Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
• [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] 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: 1495).
• [15] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [16] 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.
• [17] Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4319-21.
• [18] Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6281-7.
• [19] Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative. Bioorg Med Chem Lett. 2006 Jan 1;16(1):55-8.
• [20] Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
• [21] Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50.