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

General Information of Drug (ID: DMABZH6)

• Drug Name: PMID21561767C8h Drug Info
• Synonyms: GTPL8170; BDBM50345579

Indication

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

• Cross-matching ID:
  PubChem CID: 46864270
  TTD Drug ID: DMABZH6

Molecule-Related Drug Atlas

Drug(s) Targeting Ephrin type-A receptor 3 (EPHA3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ifabotuzumab	DMGWNCJ	Acute myeloid leukaemia	2A60	Phase 2	[2]
KB-004	DM5U3IF	Haematological malignancy	2B33.Y	Phase 1/2	[3]
PMID23489211C20	DMDYC4J	Discovery agent	N.A.	Investigative	[4]
PMID19788238C66	DMCVJK9	Discovery agent	N.A.	Investigative	[5]

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	[6]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[7]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[8]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[9]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[11]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[14]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[15]

Drug(s) Targeting Ephrin type-A receptor 7 (EPHA7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID23489211C20	DMDYC4J	Discovery agent	N.A.	Investigative	[4]
PMID19788238C66	DMCVJK9	Discovery agent	N.A.	Investigative	[5]

Drug(s) Targeting Ephrin type-A receptor 2 (EPHA2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CAR-T cells targeting EphA2	DMN3C2I	Malignant glioma	2A00.0	Phase 1/2	[16]
BT5528	DMYBKMV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[17]
DS-8895	DM31VNC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
MEDI-547	DM3WP70	Solid tumour/cancer	2A00-2F9Z	Phase 1	[19]
MEDI-543	DM7Q1PF	Solid tumour/cancer	2A00-2F9Z	Preclinical	[20]
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[21]
PMID23489211C20	DMDYC4J	Discovery agent	N.A.	Investigative	[4]
PMID19788238C66	DMCVJK9	Discovery agent	N.A.	Investigative	[5]

Drug(s) Targeting Proto-oncogene c-Ret (RET)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[22]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[23]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[23]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[24]
Selpercatinib	DMZR15V	Non-small-cell lung cancer	2C25.Y	Approved	[25]
Pralsetinib	DMWU0I2	Non-small-cell lung cancer	2C25.Y	Approved	[26]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[27]
CEP-32496	DMAO04B	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[28]
TPX-0046	DMIVE67	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[29]
GSK3179106	DM2KCIP	Inflammatory bowel disease	DD72	Phase 1	[30]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
G-1128	DMHOMFK	Chronic myelogenous leukaemia	2A20.0	Discontinued in Phase 2	[31]
PP121	DMU8KTO	Discovery agent	N.A.	Investigative	[32]
PMID24900538C2c	DM5PATM	Discovery agent	N.A.	Investigative	[33]
PMID23441572C24	DMG4MLA	Discovery agent	N.A.	Investigative	[34]
GNF-5	DMGLIPV	Discovery agent	N.A.	Investigative	[35]

Drug(s) Targeting Angiopoietin 1 receptor (TEK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AKB-9778	DMKNRYH	Diabetic macular edema	9B71.02	Phase 2	[36]
DCC-2036	DMJKFNU	Chronic myeloid leukaemia	2A20	Phase 1/2	[28]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[37]
CEP-11981	DMYDTJ6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[38]
ARRY-614	DMXD93K	Arthritis	FA20	Discontinued in Phase 1	[39]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	DMDO175	Discovery agent	N.A.	Investigative	[40]
3,4-diphenyl-1H-pyrrole-2,5-dione	DMPK6YT	Discovery agent	N.A.	Investigative	[40]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione	DMGC7RY	Discovery agent	N.A.	Investigative	[40]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione	DM3EV9N	Discovery agent	N.A.	Investigative	[40]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine	DMFO8DR	Discovery agent	N.A.	Investigative	[41]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
ABL messenger RNA (ABL mRNA)	TT6B75U	ABL1_HUMAN	Inhibitor	[1]
Angiopoietin 1 receptor (TEK)	TT9VGXW	TIE2_HUMAN	Inhibitor	[1]
Ephrin type-A receptor 2 (EPHA2)	TTRJB2G	EPHA2_HUMAN	Inhibitor	[1]
Ephrin type-A receptor 3 (EPHA3)	TTHS2LR	EPHA3_HUMAN	Inhibitor	[1]
Ephrin type-A receptor 7 (EPHA7)	TTAHTVG	EPHA7_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[1]
Proto-oncogene c-Ret (RET)	TT4DXQT	RET_HUMAN	Inhibitor	[1]

References

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• [3] Clinical pipeline report, company report or official report of Kalobios.
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• [5] 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.
• [6] 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.
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• [11] 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.
• [12] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [13] National Cancer Institute Drug Dictionary (drug id 452042).
• [14] 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.
• [15] Clinical pipeline report, company report or official report of MedImmune (2011).
• [16] ClinicalTrials.gov (NCT02575261) CAR-T Cell Immunotherapy for EphA2 Positive Malignant Glioma Patients
• [17] MMAE Delivery Using the Bicycle Toxin Conjugate BT5528. Mol Cancer Ther. 2020 Jul;19(7):1385-1394.
• [18] Clinical pipeline report, company report or official report of Daiichi Sankyo.
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• [22] Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96.
• [23] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [24] 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.
• [25] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
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• [28] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [29] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [30] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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• [33] Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. ACS Med Chem Lett. 2012 Jul 26;3(9):705-9.
• [34] Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. J Med Chem. 2013 Apr 11;56(7):3033-47.
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• [39] Cmpany report (Arraybiopharma)
• [40] Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
• [41] Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.