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

General Information of Drug (ID: DMMVHY4)

• Drug Name: Benzothiazine derivative 1 Drug Info
• Synonyms: PMID26161698-Compound-50
• Cross-matching ID:
  PubChem CID: 90074871
  TTD Drug ID: DMMVHY4

Molecule-Related Drug Atlas

Drug(s) Targeting Cyclin-dependent kinase 9 (CDK9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flavopiridol	DMKSUOI	Acute myeloid leukaemia	2A60	Phase 2	[2]
P276-00	DM9DJL2	Mantle cell lymphoma	2A85.5	Phase 2	[3]
RGB-286638	DMEGOQP	Haematological malignancy	2B33.Y	Phase 1	[4]
SNS-032	DMEITAS	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]
BTX-A51	DMC8XHQ	Advanced solid tumour	2A00-2F9Z	Phase 1	[6]
CYC065	DM9ODT6	Lymphoma	2A80-2A86	Phase 1	[2]
AZD4573	DMOYPTK	Haematological malignancy	2B33.Y	Phase 1	[2]
TP-1287	DM3Z07E	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]
VIP-152	DMBQ5OL	Chronic lymphocytic leukaemia	2A82.0	Phase 1	[8]
AZD7503	DM8XJD2	Non-alcoholic steatohepatitis	DB92.1	Phase 1	[9]

Drug(s) Targeting Serine/threonine-protein kinase pim-1 (PIM1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SEL-24	DMH064K	Acute myeloid leukaemia	2A60	Phase 1/2	[10]
CXR-1002	DM4GJ50	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
leucettine L41	DMBYND6	Discovery agent	N.A.	Investigative	[12]
PMID21982499C14k	DM0VOXN	Discovery agent	N.A.	Investigative	[13]
PMID22136433C20	DMI8217	Discovery agent	N.A.	Investigative	[14]
NCGC00167772-01	DMY8RT9	Discovery agent	N.A.	Investigative	[10]
SMI-4a	DMBLWMS	Non-small-cell lung cancer	2C25	Investigative	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cyclin-dependent kinase 9 (CDK9)	TT1LVF2	CDK9_HUMAN	Inhibitor	[1]
Serine/threonine-protein kinase pim-1 (PIM1)	TTTN5QW	PIM1_HUMAN	Inhibitor	[1]

References

• [1] Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
• [2] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [3] Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
• [4] Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75.
• [5] Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45.
• [6] Clinical pipeline report, company report or official report of BioTheryX.
• [7] Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
• [8] VIP152 is a selective CDK9 inhibitor with pre-clinical in vitro and in vivo efficacy in chronic lymphocytic leukemia. Leukemia. 2023 Feb;37(2):326-338.
• [9] ClinicalTrials.gov (NCT05560607) An Open-label, Non-randomized, Multiple-dose Study to Assess the Knockdown of Hepatic HSD17B13 mRNA Expression, Pharmacokinetics, Safety, and Tolerability Following Administration of AZD7503 in Participants With Non-alcoholic Fatty Liver Disease. U.S.National Institutes of Health.
• [10] 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: 2158).
• [11] 123 Antitumor activity of CXR1002, a novel anti-cancer clinical phase compound that induces ER stress and inhibits PIM kinases: Human tumor xenograft efficacy and in vitro mode of action. EJC Supplements, 2010; 8(7):45-46.
• [12] Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem. 2011 Jun 23;54(12):4172-86.
• [13] 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6687-92.
• [14] 7,8-dichloro-1-oxo-beta-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem. 2012 Jan 12;55(1):403-13.
• [15] Pim-1 inhibitor SMI-4a suppresses tumor growth in non-small cell lung cancer via PI3K/AKT/mTOR pathway. Onco Targets Ther. 2019 Apr 23;12:3043-3050.