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

General Information of Drug (ID: DMNM63G)

• Drug Name: BTP2 Drug Info
• Synonyms: YM-58483

Indication

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

• Cross-matching ID:
  PubChem CID: 2455
  CAS Number: CAS 223499-30-7
  TTD Drug ID: DMNM63G

Molecule-Related Drug Atlas

Drug(s) Targeting Short transient receptor potential channel 5 (TRPC5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BI 1358894	DM740BS	Depression	6A70-6A7Z	Phase 2	[5]
GFB-887	DM2IJWG	Diabetic nephropathy	GB61.Z	Phase 2	[6]
2-APB	DM9AKVR	Discovery agent	N.A.	Investigative	[7]
daidzein	DMRFTJX	Discovery agent	N.A.	Investigative	[4]
lysophosphatidylcholine	DMOGFVH	Discovery agent	N.A.	Investigative	[4]
KB-R7943	DMMD5W3	Discovery agent	N.A.	Investigative	[8]
bromoenol lactone	DMKQ0CA	Discovery agent	N.A.	Investigative	[9]
ML204	DM15YL0	Discovery agent	N.A.	Investigative	[10]
(-)-englerin A	DMPQBWY	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Short transient receptor potential channel 3 (TRPC3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-APB	DM9AKVR	Discovery agent	N.A.	Investigative	[12]
ACAA	DMACYPW	Discovery agent	N.A.	Investigative	[13]
OAG	DMOP8IJ	Discovery agent	N.A.	Investigative	[14]
KB-R7943	DMMD5W3	Discovery agent	N.A.	Investigative	[13]
Pyr3	DM3VNYQ	Discovery agent	N.A.	Investigative	[15]

Drug(s) Targeting Long transient receptor potential channel 4 (TRPM4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[16]
PIP2	DMOZV7N	Discovery agent	N.A.	Investigative	[17]
adenosine diphosphate	DMFUHKP	N. A.	N. A.	Investigative	[16]
decavanadate	DMLT1N3	Discovery agent	N.A.	Investigative	[18]
9-phenanthrol	DMJFBQ1	Discovery agent	N.A.	Investigative	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Long transient receptor potential channel 4 (TRPM4)	TTJ2HKA	TRPM4_HUMAN	Activator	[2]
Short transient receptor potential channel 3 (TRPC3)	TTNVC34	TRPC3_HUMAN	Blocker (channel blocker)	[3]
Short transient receptor potential channel 5 (TRPC5)	TT32NQ1	TRPC5_HUMAN	Blocker (channel blocker)	[4]

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. (Ligand id: 2438).
• [2] A pyrazole derivative potently inhibits lymphocyte Ca2+ influx and cytokine production by facilitating transient receptor potential melastatin 4 ch... Mol Pharmacol. 2006 Apr;69(4):1413-20.
• [3] A functional link between store-operated and TRPC channels revealed by the 3,5-bis(trifluoromethyl)pyrazole derivative, BTP2. J Biol Chem. 2005 Mar 25;280(12):10997-1006.
• [4] 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: 490).
• [5] Clinical pipeline report, company report or official report of Boehringer Ingelheim.
• [6] Safety and Efficacy of GFB-887, a TRPC5 Channel Inhibitor, in Patients With Focal Segmental Glomerulosclerosis, Treatment-Resistant Minimal Change Disease, or Diabetic Nephropathy: TRACTION-2 Trial Design. Kidney Int Rep. 2021 Jul 23;6(10):2575-2584.
• [7] Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol. 2005 Jun;145(4):405-14.
• [8] The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels. Biochem Biophys Res Commun. 2007 Sep 14;361(1):230-6.
• [9] Bromoenol lactone inhibits voltage-gated Ca2+ and transient receptor potential canonical channels. J Pharmacol Exp Ther. 2011 Nov;339(2):329-40.
• [10] Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46.
• [11] (-)-Englerin is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.
• [12] Mechanism of inhibition of TRPC cation channels by 2-aminoethoxydiphenylborane. Mol Pharmacol. 2005 Sep;68(3):758-62.
• [13] 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: 488).
• [14] Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol. Nature. 1999 Jan 21;397(6716):259-63.
• [15] Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5400-5.
• [16] Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b. Pflugers Arch. 2004 Apr;448(1):70-5.
• [17] Phosphatidylinositol 4,5-bisphosphate rescues TRPM4 channels from desensitization. J Biol Chem. 2005 Nov 25;280(47):39185-92.
• [18] Decavanadate modulates gating of TRPM4 cation channels. J Physiol. 2004 Nov 1;560(Pt 3):753-65.
• [19] 9-phenanthrol inhibits human TRPM4 but not TRPM5 cationic channels. Br J Pharmacol. 2008 Apr;153(8):1697-705.