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

General Information of Drug (ID: DMNB4XK)

• Drug Name: BVD-523 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Melanoma	2C30	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[2]
Pancreatic cancer	2C10	Phase 1	[3]

• Cross-matching ID:
  PubChem CID: 11719003
  CAS Number: CAS 869886-67-9
  TTD Drug ID: DMNB4XK

Molecule-Related Drug Atlas

Drug(s) Targeting Extracellular signal-regulated kinase 1 (ERK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HH2710	DM0C5MV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[5]
ASTX029	DMVZXIA	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[6]
VAN-10-4-eluting stent	DM3ZW6A	Artery stenosis	BD52	Phase 1	[7]
GDC-0994	DMFC2OY	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
JSI-1187	DMVJWBS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
ASN007	DMYHEUA	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
COR-D	DMLXMCB	T-cell leukaemia	2A90	Preclinical	[10]
6-[(E)-2-(4-Fluoro-phenyl)-vinyl]-9H-purine	DMDNG8F	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Extracellular signal-regulated kinase 2 (ERK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
HH2710	DM0C5MV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[5]
ASTX029	DMVZXIA	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[6]
VAN-10-4-eluting stent	DM3ZW6A	Artery stenosis	BD52	Phase 1	[7]
GDC-0994	DMFC2OY	Solid tumour/cancer	2A00-2F9Z	Phase 1	[8]
JSI-1187	DMVJWBS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[9]
LY3214996	DMFDAY7	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
CHIR-99021	DMB8MNU	Allergic inflammation	4A80-4A85	Patented	[12]
COR-D	DMLXMCB	T-cell leukaemia	2A90	Preclinical	[10]
SB220025	DMSBUET	Arthritis	FA20	Terminated	[13]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[14]

Drug(s) Targeting Ephrin type-B receptor 2 (EPHB2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SEphB4-HSA	DMD8RU0	Kaposi sarcoma	2B57	Phase 2	[15]
KO-947	DMZMSBI	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
MK-8353	DMLCTI5	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[16]
PMID23489211C20	DMDYC4J	Discovery agent	N.A.	Investigative	[17]
PMID19788238C66	DMCVJK9	Discovery agent	N.A.	Investigative	[18]
SNEWIQPRLPQH	DMYUH62	Discovery agent	N.A.	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Ephrin type-B receptor 2 (EPHB2)	TTKPV6O	EPHB2_HUMAN	Inhibitor	[3]
Extracellular signal-regulated kinase 1 (ERK1)	TT1MG9E	MK03_HUMAN	Modulator	[4]
Extracellular signal-regulated kinase 2 (ERK2)	TT4TQBX	MK01_HUMAN	Modulator	[4]

References

• [1] ClinicalTrials.gov (NCT03417739) A Phase II Study of BVD-523 in Metastatic Uveal Melanoma. U.S. National Institutes of Health.
• [2] ClinicalTrials.gov (NCT01781429) Phase I Dose-Escalation, Safety, Pharmacokinetic and Pharmacodynamic Study of BVD-523 in Patients With Advanced Malignancies. U.S. National Institutes of Health.
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] DOI: 10.1158/1538-7445.AM2015-4693
• [5] Clinical pipeline report, company report or official report of HaiHe Biopharma.
• [6] Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
• [7] WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
• [8] ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
• [9] National Cancer Institute Drug Dictionary (drug name JSI1187).
• [10] 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.
• [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] 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.
• [13] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [14] Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
• [15] National Cancer Institute Drug Dictionary (drug name SEphB4-HSA).
• [16] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [17] Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. J Med Chem. 2013 Apr 11;56(7):2936-47.
• [18] Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem. 2009 Oct 22;52(20):6433-46.
• [19] Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition. J Biol Chem. 2007 Dec 14;282(50):36505-13.