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

General Information of Drug (ID: DMMD5W3)

Drug Name
KB-R7943 Drug Info
Synonyms
182004-65-5; KB-R7943 mesylate; KB-R7943; 2-[2-[4-(4-NITROBENZYLOXY)PHENYL]ETHYL]ISOTHIOUREA MESYLATE; KB-R7943 (mesylate); 4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioate methanesulfonate; 4-((4-Nitrobenzyl)oxy)phenethyl carbamimidothioatemethanesulfonate; 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate; 4-[(4-Nitrobenzyl)oxy]phenethyl Carbamimidothioate Methanesulfonate; KB-R7943 mesylate; SCHEMBL742683; GTPL4232; CTK0H1228; DTXSID50431360; MolPort-003-983-603; C16H17N3O3S.CH4O3S; HMS3267H09
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9823846
CAS Number
CAS 182004-65-5
TTD Drug ID
DMMD5W3

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Download the Complete Related Drug List
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 [8]
lysophosphatidylcholine DMOGFVH Discovery agent N.A. Investigative [8]
BTP2 DMNM63G 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]
⏷ Show the Full List of 9 Drug(s)
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 [2]
OAG DMOP8IJ Discovery agent N.A. Investigative [13]
BTP2 DMNM63G Discovery agent N.A. Investigative [14]
Pyr3 DM3VNYQ Discovery agent N.A. Investigative [15]
Drug(s) Targeting Short transient receptor potential channel 6 (TRPC6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-APB DM9AKVR Discovery agent N.A. Investigative [4]
lysophosphatidylcholine DMOGFVH Discovery agent N.A. Investigative [4]
ACAA DMACYPW Discovery agent N.A. Investigative [4]
OAG DMOP8IJ Discovery agent N.A. Investigative [13]
flufenamate DMN8AP0 Discovery agent N.A. Investigative [4]
SAG DMHOG7W Discovery agent N.A. Investigative [13]
ML9 DMP13VE Discovery agent N.A. Investigative [4]
hyp 9 DM0U8IV Discovery agent N.A. Investigative [16]
SLG DMEBPCO Discovery agent N.A. Investigative [13]
20-HETE DM5BAJ9 Discovery agent N.A. Investigative [4]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Short transient receptor potential channel 3 (TRPC3) TTNVC34 TRPC3_HUMAN Blocker (channel blocker) [2]
Short transient receptor potential channel 5 (TRPC5) TT32NQ1 TRPC5_HUMAN Blocker (channel blocker) [3]
Short transient receptor potential channel 6 (TRPC6) TTRBT3W TRPC6_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: 4232).
2 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).
3 The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels. Biochem Biophys Res Commun. 2007 Sep 14;361(1):230-6.
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: 491).
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 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).
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 Direct activation of human TRPC6 and TRPC3 channels by diacylglycerol. Nature. 1999 Jan 21;397(6716):259-63.
14 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.
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 Simple 2,4-diacylphloroglucinols as classic transient receptor potential-6 activators--identification of a novel pharmacophore. Mol Pharmacol. 2010 Mar;77(3):368-77.