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

General Information of Drug (ID: DM5DMCH)

• Drug Name: Ro-4396686 Drug Info
• Synonyms: SCHEMBL5809947; CHEMBL606964

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 11396738
  TTD Drug ID: DM5DMCH

Molecule-Related Drug Atlas

Drug(s) Targeting Fyn tyrosine protein kinase (FYN)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dasatinib	DMJV2EK	Chronic myelogenous leukaemia	2A20.0	Approved	[2]
JNJ-26483327	DMSQ3AZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]
PMID15546730C2	DMOPUIH	Discovery agent	N.A.	Investigative	[4]
CEP-5104	DMV43GY	Discovery agent	N.A.	Investigative	[5]
CEP-6331	DMNXBTD	Discovery agent	N.A.	Investigative	[5]
JNJ-10198409	DM9GDP5	Discovery agent	N.A.	Investigative	[6]
1-Methoxy-2-[2-(2-Methoxy-Ethoxy]-Ethane	DMD7WNV	Discovery agent	N.A.	Investigative	[7]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
VFEDEOUBYBLDKN-AAFJCEBUSA-N	DMH9ION	N. A.	N. A.	Patented	[8]
XHPNYYOUZWOWNT-PYUWXLGESA-N	DM5Q93Y	N. A.	N. A.	Patented	[8]
AGGGWZCOULSEER-PYUWXLGESA-N	DM2L83Y	N. A.	N. A.	Patented	[8]
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[9]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[10]
NM-PP1	DMS8H5Q	Discovery agent	N.A.	Investigative	[11]
ISIS 102633	DMWT7BK	Discovery agent	N.A.	Investigative	[12]
ISIS 102604	DMZ6X9B	Discovery agent	N.A.	Investigative	[12]
ISIS 102619	DMXH9IT	Discovery agent	N.A.	Investigative	[12]
ISIS 102462	DMXNC0B	Discovery agent	N.A.	Investigative	[12]

Drug(s) Targeting FGFR4 messenger RNA (FGFR4 mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ISIS-FGFR4	DMNVZDT	Obesity	5B81	Phase 2	[13]
FGF401	DMWEJ0C	Hepatocellular carcinoma	2C12.02	Phase 1/2	[14]
H3B-6527	DMAYTRK	Hepatocellular carcinoma	2C12.02	Phase 1	[14]
BLU-554	DM27J3D	Hepatocellular carcinoma	2C12.02	Phase 1	[14]
PD-0183812	DMWYP86	Retinoblastoma	2D02.2	Terminated	[15]

Drug(s) Targeting Fibroblast growth factor receptor 1 (FGFR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[16]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[17]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[18]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[20]
Rosiglitazone + metformin	DMPIDXT	Diabetic complication	5A2Y	Phase 3	[2]
BGJ398	DMNKBEC	Cholangiocarcinoma	2C12.10	Phase 3	[21]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[22]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[23]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]

Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[24]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[25]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[26]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[27]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[28]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[29]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[30]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[31]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[32]

Drug(s) Targeting Fibroblast growth factor receptor 2 (FGFR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[18]
Interferon Alfa-2a, Recombinant	DMUTZ8S	Chronic HCV-1 infection	1E51.1	Approved	[33]
Palifermin	DM9JOYP	Oral mucositis	DA01.11	Approved	[34]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
Trafermin	DMLKI2B	Periodontitis	DA0C	Phase 3	[35]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
LY2874455	DMZ0DMY	Solid tumour/cancer	2A00-2F9Z	Phase 2	[36]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[37]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[2]
BAY1179470	DM7L91K	Solid tumour/cancer	2A00-2F9Z	Phase 1	[38]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BVD-523	DMNB4XK	Melanoma	2C30	Phase 2	[39]
HH2710	DM0C5MV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[40]
ASTX029	DMVZXIA	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[41]
VAN-10-4-eluting stent	DM3ZW6A	Artery stenosis	BD52	Phase 1	[42]
GDC-0994	DMFC2OY	Solid tumour/cancer	2A00-2F9Z	Phase 1	[43]
JSI-1187	DMVJWBS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[44]
LY3214996	DMFDAY7	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
CHIR-99021	DMB8MNU	Allergic inflammation	4A80-4A85	Patented	[45]
COR-D	DMLXMCB	T-cell leukaemia	2A90	Preclinical	[46]
SB220025	DMSBUET	Arthritis	FA20	Terminated	[7]

Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[47]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[24]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[48]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[29]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[30]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[37]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[49]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[50]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[51]

Drug(s) Targeting Epidermal growth factor receptor (EGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[52]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[53]
Gefitinib	DM15F0X	Solid tumour/cancer	2A00-2F9Z	Approved	[54]
Erlotinib	DMCMBHA	Non-small-cell lung cancer	2C25.Y	Approved	[55]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[2]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[56]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[57]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[58]
Epidermal growth factor	DMVONE6	Vulnerary	ND56.Z	Approved	[56]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[59]

Drug(s) Targeting cAMP protein kinase type II-beta (PRKAR2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[9]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[10]
[3H]cAMP	DMZRQU7	Discovery agent	N.A.	Investigative	[7]
AdoC(Dpr)2AlaArg6	DM2TWSZ	Discovery agent	N.A.	Investigative	[60]
AdcAhxArg4NH(CH2)6NH2	DMSYMRJ	Discovery agent	N.A.	Investigative	[61]
AdcAhxArg4Lys-PEGOMe	DMQ2C8X	Discovery agent	N.A.	Investigative	[61]
AdoC(GABA)Arg6	DMMWNPT	Discovery agent	N.A.	Investigative	[60]
AdcAhxArg4Lys(biotin)-PEG-OMe	DMZYJHV	Discovery agent	N.A.	Investigative	[61]
AdoC(Aun)Arg6	DMDLHAB	Discovery agent	N.A.	Investigative	[60]
AdoCGlyArg6	DMVQJP0	Discovery agent	N.A.	Investigative	[60]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[47]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[16]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[62]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[63]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[64]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[2]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[65]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[66]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[67]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[68]

Drug(s) Targeting Fungal Protein kinase A (Fung ypkA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[9]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[10]
PMID20005102C1	DMMESBW	Discovery agent	N.A.	Investigative	[69]
[3H]cAMP	DMZRQU7	Discovery agent	N.A.	Investigative	[70]
PMID19364658C33	DMSE1C3	Discovery agent	N.A.	Investigative	[71]
BX-912	DMZA45C	Discovery agent	N.A.	Investigative	[72]
BX-795	DMRIMLJ	Discovery agent	N.A.	Investigative	[72]
Chelerythrine	DMCP1G9	Discovery agent	N.A.	Investigative	[73]
PMID21742770C1	DME3JMH	Discovery agent	N.A.	Investigative	[74]
Rp-adenosine 3',5'-cyclic monophosphothioate triethylamine (Rp-cAMPS)	DM1JWGH	Discovery agent	N.A.	Investigative	[75]

Drug(s) Targeting Fibroblast growth factor receptor 3 (FGFR3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[18]
Trapidil	DMY67U8	Acute coronary syndrome	BA41	Phase 4	[76]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[19]
TKI258	DMYLT67	Renal cell carcinoma	2C90	Phase 3	[2]
BMS-582664	DMDAN8H	Hepatocellular carcinoma	2C12.02	Phase 3	[2]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
B-701	DMOMDA4	Bladder cancer	2C94	Phase 2	[77]
Recifercept	DML8N3Y	Achondroplasia	LD24.00	Phase 2	[78]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[37]
AEE-788	DMEOS5K	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[2]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
cAMP protein kinase type II-beta (PRKAR2B)	TTW4Y2M	KAP3_HUMAN	Inhibitor	[1]
Epidermal growth factor receptor (EGFR)	TTGKNB4	EGFR_HUMAN	Inhibitor	[1]
Extracellular signal-regulated kinase 2 (ERK2)	TT4TQBX	MK01_HUMAN	Inhibitor	[1]
FGFR4 messenger RNA (FGFR4 mRNA)	TT1KX2S	FGFR4_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 2 (FGFR2)	TTGJVQM	FGFR2_HUMAN	Inhibitor	[1]
Fibroblast growth factor receptor 3 (FGFR3)	TTST7KB	FGFR3_HUMAN	Inhibitor	[1]
Fungal Protein kinase A (Fung ypkA)	TTYVI76	Q56921_YEREN	Inhibitor	[1]
Fyn tyrosine protein kinase (FYN)	TT2B9KF	FYN_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[1]
PRKACA messenger RNA (PRKACA mRNA)	TT5U49F	KAPCA_HUMAN	Inhibitor	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[1]

References

• [1] Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
• [2] 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.
• [3] National Cancer Institute Drug Dictionary (drug id 596693).
• [4] Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6.
• [5] Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9.
• [6] (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad ant... J Med Chem. 2005 Dec 29;48(26):8163-73.
• [7] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [8] Purine derivatives. US8846696.
• [9] Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address
• [10] 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.
• [11] The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
• [12] US patent application no. 6,248,586, Antisense modulation of PKA catalytic subunit C-alpha expression.
• [13] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011).
• [14] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [15] Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.
• [16] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [17] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [18] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [19] E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
• [20] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [21] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [22] 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: 1808).
• [23] AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
• [24] Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
• [25] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [26] A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
• [27] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [28] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
• [29] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [30] National Cancer Institute Drug Dictionary (drug id 452042).
• [31] Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
• [32] Clinical pipeline report, company report or official report of MedImmune (2011).
• [33] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [34] Keratinocyte growth factor. Expert Opin Biol Ther. 2009 Jun;9(6):779-87.
• [35] Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
• [36] Company report (Eli Lilly) (drug: LY2874455)
• [37] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [38] National Cancer Institute Drug Dictionary (drug id 751593).
• [39] DOI: 10.1158/1538-7445.AM2015-4693
• [40] Clinical pipeline report, company report or official report of HaiHe Biopharma.
• [41] Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
• [42] WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
• [43] ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
• [44] National Cancer Institute Drug Dictionary (drug name JSI1187).
• [45] 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.
• [46] 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.
• [47] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [48] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [49] Company report (Neuronova)
• [50] Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
• [51] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [52] Nasopharyngeal carcinoma: Current treatment options and future directions. J Nasopharyng Carcinoma, 2014, 1(16): e16.
• [53] Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
• [54] Gefitinib ('Iressa', ZD1839) and new epidermal growth factor receptor inhibitors. Br J Cancer. 2004 Feb 9;90(3):566-72.
• [55] Quantitative prediction of fold resistance for inhibitors of EGFR. Biochemistry. 2009 Sep 8;48(35):8435-48.
• [56] 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: 1797).
• [57] Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
• [58] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [59] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [60] Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases. Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.
• [61] Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3035-9.
• [62] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [63] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [64] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [65] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [66] Clinical pipeline report, company report or official report of Exelixis (2011).
• [67] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [68] Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
• [69] 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.
• [70] 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: 1694).
• [71] 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.
• [72] Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
• [73] A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
• [74] A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett. 2012 Dec 13;3(12):1034-1038.
• [75] Inhibition of protein kinase A activity interferes with long-term, but not short-term, memory of conditioned taste aversions. Behav Neurosci. 2002 Dec;116(6):1070-4.
• [76] Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
• [77] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [78] In vitro and in vivo characterization of Recifercept, a soluble fibroblast growth factor receptor 3, as treatment for achondroplasia. PLoS One. 2020 Dec 28;15(12):e0244368.