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

General Information of Drug (ID: DMZG1L5)

• Drug Name: PLX-ORI3 Drug Info
• Synonyms: Omni-Raf inhibitors (cancer); Omni-Raf inhibitors (cancer), Plexxikon

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Investigative	[1]

• Cross-matching ID: TTD Drug ID: DMZG1L5

Molecule-Related Drug Atlas

Drug(s) Targeting Raf messenger RNA (Raf mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MLN2480	DMBR8NF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]
RG7304	DMGFAVQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
SPN-803	DM8O2AQ	Parkinson disease	8A00.0	Phase 1	[2]
LXH254	DMQE9PS	Non-small-cell lung cancer	2C25.Y	Phase 1	[4]
ICo-007	DM79W8K	Diabetic macular edema	9B71.02	Phase 1	[5]
LErafAON	DMNHPOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
DEBROMOHYMENIALDISINE	DMDLER8	Discovery agent	N.A.	Investigative	[7]
ZM-336372	DMD5JYQ	Discovery agent	N.A.	Investigative	[8]
6-[(E)-2-(4-Fluoro-phenyl)-vinyl]-9H-purine	DMDNG8F	Discovery agent	N.A.	Investigative	[9]
6-Benzylsulfanyl-9H-purine	DMI7FNZ	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting B-Raf messenger RNA (BRAF mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MLN2480	DMBR8NF	Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]
RG7304	DMGFAVQ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
SPN-803	DM8O2AQ	Parkinson disease	8A00.0	Phase 1	[1]
PLX-4720	DMBK9AM	Cutaneous melanoma	2C30	Phase 1	[10]
L-779450	DM51B74	Discovery agent	N.A.	Investigative	[11]
ZM-336372	DMD5JYQ	Discovery agent	N.A.	Investigative	[8]
2-(Phenylamino)-6-(3-acetamidophenyl)pyrazine	DMPUARE	Discovery agent	N.A.	Investigative	[12]
ISIS 13741	DMC7Q38	Discovery agent	N.A.	Investigative	[13]
ISIS 14144	DMWIKD5	Discovery agent	N.A.	Investigative	[13]
PMID26061392C2	DMHZOIU	Discovery agent	N.A.	Investigative	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
B-Raf messenger RNA (BRAF mRNA)	TT0EOB8	BRAF_HUMAN	Inhibitor	[1]
Raf messenger RNA (Raf mRNA)	TTAN5W2	RAF1_HUMAN	Inhibitor	[2]

References

• [1] 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: 1943).
• [2] 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: 2184).
• [3] Clinical pipeline report, company report or official report of Roche.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2009).
• [6] Combination with liposome-entrapped, ends-modified raf antisense oligonucleotide (LErafAON) improves the anti-tumor efficacies of cisplatin, epirubicin, mitoxantrone, docetaxel and gemcitabine. Anticancer Drugs. 2004 Mar;15(3):243-53.
• [7] Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1). J Med Chem. 2002 Jan 17;45(2):529-32.
• [8] The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
• [9] Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
• [10] Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51.
• [11] The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.
• [12] Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead. J Med Chem. 2006 Jan 12;49(1):407-16.
• [13] US patent application no. 5,981,731, Antisense oligonucleotide modulation of B-raf gene expression.
• [14] Photoactivatable Prodrugs of Antimelanoma Agent Vemurafenib. ACS Chem Biol. 2015 Sep 18;10(9):2099-107.