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

General Information of Drug (ID: DMK3SAF)

• Drug Name: BI-D1870 Drug Info
• Synonyms: 501437-28-1; 2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one; 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one; C19H23F2N5O2; 2-(3,5-difluoro-4-hydroxyphenylamino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one; BI-D 1870; CHEMBL573107; GTPL8038; SCHEMBL13881333; CTK8I8998; BDBM25017; DTXSID40648506; BID1870; MolPort-008-266-821; HMS3244D11; HMS3244C12; HMS3244C11; BCPP000343; HMS3651D17; BCP01977; EX-A2471; NSC747342

Indication

Disease Entry	ICD 11	Status	REF
Chronic lymphocytic leukaemia	2A82.0	Preclinical	[1]

• Cross-matching ID:
  PubChem CID: 25023738
  CAS Number: CAS 501437-28-1
  TTD Drug ID: DMK3SAF

Molecule-Related Drug Atlas

Drug(s) Targeting Ribosomal protein S6 kinase alpha-3 (RSK3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID27410995-Compound-Figure3j	DMJRZLB	N. A.	N. A.	Patented	[2]
Indole-based analog 14	DMQURWZ	N. A.	N. A.	Patented	[2]
Pyrrolo[2,3-d]pyrimidine derivative 35	DMXU08A	N. A.	N. A.	Patented	[2]
PMID22765894C8h	DMH5RFU	Discovery agent	N.A.	Investigative	[3]
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[4]
BIX 02565	DMNAX1Q	Discovery agent	N.A.	Investigative	[5]

Drug(s) Targeting Ribosomal protein S6 kinase alpha-2 (RSK2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[4]

Drug(s) Targeting Ribosomal protein S6 kinase alpha-1 (RSK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,6-diazanaphthalenes and pyrido[2,3-d] pyrimidine derivative 1	DMUQ9CF	N. A.	N. A.	Patented	[2]
Heterocyclic derivative 26	DM56T1P	N. A.	N. A.	Patented	[2]
1,6-diazanaphthalenes and pyrido[2,3-d] pyrimidine derivative 2	DMPZ0U8	N. A.	N. A.	Patented	[2]
Pyrrolo[2,3-d]pyrimidine derivative 1	DMYUEA6	N. A.	N. A.	Patented	[2]
Pyrrolo[2,3-d]pyrimidine derivative 2	DMJFYK1	N. A.	N. A.	Patented	[2]
PMID19364658C33	DMSE1C3	Discovery agent	N.A.	Investigative	[6]
GSK-1838705A	DM4HLK3	Discovery agent	N.A.	Investigative	[7]

Drug(s) Targeting Ribosomal protein S6 kinase alpha-6 (RSK6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US10081632, Compound 25	DM3BDHN	N. A.	N. A.	Patented	[8]
CID 138805970	DMINXMY	N. A.	N. A.	Patented	[8]
PMID22564207C25b	DMBMYKQ	Discovery agent	N.A.	Investigative	[4]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Ribosomal protein S6 kinase alpha-1 (RSK1)	TTIXKA4	KS6A1_HUMAN	Inhibitor	[1]
Ribosomal protein S6 kinase alpha-2 (RSK2)	TT0ZW9O	KS6A2_HUMAN	Inhibitor	[1]
Ribosomal protein S6 kinase alpha-3 (RSK3)	TTUM2ZR	KS6A3_HUMAN	Inhibitor	[1]
Ribosomal protein S6 kinase alpha-6 (RSK6)	TT3KYWB	KS6A6_HUMAN	Inhibitor	[1]

References

• [1] BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J. 2007 Jan 1;401(1):29-38.
• [2] Ribosomal S6 kinase (RSK) modulators: a patent review.Expert Opin Ther Pat. 2016 Sep;26(9):1061-78.
• [3] The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
• [4] Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J Med Chem. 2012 May 24;55(10):4580-93.
• [5] Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42.
• [6] 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.
• [7] GSK1838705A inhibits the insulin-like growth factor-1 receptor and anaplastic lymphoma kinase and shows antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2009 Oct;8(10):2811-20.
• [8] Substituted tetrahydropyrido[3,2:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors. US9771366.