General Information of Drug (ID: DMPQBWY)

Drug Name
(-)-englerin A Drug Info
Synonyms Englerin A; (-)-englerin A; CHEBI:72441; (1R,3aR,4S,5R,7R,8S,8aR)-5-(glycoloyloxy)-7-isopropyl-1,4-dimethyldecahydro-4,7-epoxyazulen-8-yl (2E)-3-phenylacrylate; GTPL8372; SCHEMBL12280306
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
46242512
ChEBI ID
CHEBI:72441
TTD Drug ID
DMPQBWY

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BI 1358894 DM740BS Depression 6A70-6A7Z Phase 2 [3]
GFB-887 DM2IJWG Diabetic nephropathy GB61.Z Phase 2 [4]
2-APB DM9AKVR Discovery agent N.A. Investigative [5]
daidzein DMRFTJX Discovery agent N.A. Investigative [6]
lysophosphatidylcholine DMOGFVH Discovery agent N.A. Investigative [6]
KB-R7943 DMMD5W3 Discovery agent N.A. Investigative [7]
BTP2 DMNM63G Discovery agent N.A. Investigative [6]
bromoenol lactone DMKQ0CA Discovery agent N.A. Investigative [8]
ML204 DM15YL0 Discovery agent N.A. Investigative [9]
⏷ Show the Full List of 9 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BI 1358894 DM740BS Depression 6A70-6A7Z Phase 2 [3]
2-APB DM9AKVR Discovery agent N.A. Investigative [10]
ML204 DM15YL0 Discovery agent N.A. Investigative [9]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Short transient receptor potential channel 4 (TRPC4) TTX0H5W TRPC4_HUMAN Agonist [2]
Short transient receptor potential channel 5 (TRPC5) TT32NQ1 TRPC5_HUMAN Agonist [2]

References

1 Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
2 (-)-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.
3 Clinical pipeline report, company report or official report of Boehringer Ingelheim.
4 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.
5 Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect. Br J Pharmacol. 2005 Jun;145(4):405-14.
6 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).
7 The Na+/Ca2+ exchange inhibitor KB-R7943 potently blocks TRPC channels. Biochem Biophys Res Commun. 2007 Sep 14;361(1):230-6.
8 Bromoenol lactone inhibits voltage-gated Ca2+ and transient receptor potential canonical channels. J Pharmacol Exp Ther. 2011 Nov;339(2):329-40.
9 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.
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: 489).