General Information of Drug (ID: DMOZV7N)

Drug Name
PIP2 Drug Info
Synonyms phosphatidylinositol-4,5-bisphosphate
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
5311358
TTD Drug ID
DMOZV7N
VARIDT Drug ID
DR01018

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Preclinical Drug(s)
Drug(s) Targeting Phospholipase D2 (PLD2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
VU0364739 DMOI0TN Coagulation defect 3B10.0 Clinical trial [12]
Drug Name Drug ID Indication ICD 11 Highest Status REF
2-APB DM9AKVR Discovery agent N.A. Investigative [13]
carvacrol DMINM2D Discovery agent N.A. Investigative [14]
waixenicin A DMB6H35 Discovery agent N.A. Investigative [15]
Drug Name Drug ID Indication ICD 11 Highest Status REF
F3 DM69MKU Discovery agent N.A. Investigative [16]
Drug Name Drug ID Indication ICD 11 Highest Status REF
ML297 DMY40UG Discovery agent N.A. Investigative [17]
Drug Name Drug ID Indication ICD 11 Highest Status REF
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [18]
zinc pyrithione DMF0CRA Discovery agent N.A. Investigative [19]
XE991 DMLH1PK Discovery agent N.A. Investigative [20]
(S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide DMGFOQJ Discovery agent N.A. Investigative [21]
NC00075159 DMJCYMW Discovery agent N.A. Investigative [22]
ML213 DMFAUGP Discovery agent N.A. Investigative [23]
⏷ Show the Full List of 6 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
decavanadate DMLT1N3 Discovery agent N.A. Investigative [7]
inositol 2,4,5-trisphosphate DM43G5Z Discovery agent N.A. Investigative [7]
xestospongin C DM4YQR2 Discovery agent N.A. Investigative [7]
Drug Name Drug ID Indication ICD 11 Highest Status REF
cyclic CMP DMVJL8H Discovery agent N.A. Investigative [24]
Drug Name Drug ID Indication ICD 11 Highest Status REF
ICA-69673 DM1RZVI Pain MG30-MG3Z Preclinical [25]
[14C]TEA DM6SFYH Discovery agent N.A. Investigative [26]
PD-32577 DMBA15J Discovery agent N.A. Investigative [27]
zinc pyrithione DMF0CRA Discovery agent N.A. Investigative [19]
XE991 DMLH1PK Discovery agent N.A. Investigative [28]
(S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide DMGFOQJ Discovery agent N.A. Investigative [21]
QO-58 DMYXPF8 Discovery agent N.A. Investigative [29]
ICA-27243 DMO0N3Q Discovery agent N.A. Investigative [30]
ztz240 DM60N3C Discovery agent N.A. Investigative [31]
⏷ Show the Full List of 9 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
oleoyl-CoA DMJ1VRU Discovery agent N.A. Investigative [32]
Drug Name Drug ID Indication ICD 11 Highest Status REF
phorbol 12-myristate 13-acetate DMJWD62 Acute myeloid leukaemia 2A60 Phase 2 [33]
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMP-PNP DMTOK1D Discovery agent N.A. Investigative [34]
adenosine diphosphate DMFUHKP N. A. N. A. Investigative [34]
decavanadate DMLT1N3 Discovery agent N.A. Investigative [35]
BTP2 DMNM63G Discovery agent N.A. Investigative [36]
9-phenanthrol DMJFBQ1 Discovery agent N.A. Investigative [37]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Hyperpolarization cyclic nucleotide-gated channel 2 (HCN2) TT9EUT4 HCN2_HUMAN Activator [2]
Inward rectifier potassium channel Kir2.1 (KCNJ2) TTH7UO3 KCNJ2_HUMAN Activator [3]
Inward rectifier potassium channel Kir3.1 (KCNJ3) TTGM19J KCNJ3_HUMAN Activator [4]
Inward rectifier potassium channel Kir3.2 (KCNJ6) TTTIBVP KCNJ6_HUMAN Activator [4]
Inward rectifier potassium channel Kir3.3 (KCNJ9) TT4VHL6 KCNJ9_HUMAN Activator [5]
Inward rectifier potassium channel Kir3.4 (KCNJ5) TTEO25X KCNJ5_HUMAN Activator [6]
IP3 receptor isoform 1 (ITPR1) TT5HWAT ITPR1_HUMAN Antagonist [7]
Long transient receptor potential channel 4 (TRPM4) TTJ2HKA TRPM4_HUMAN Activator [8]
Long transient receptor potential channel 7 (TRPM7) TTFPVZO TRPM7_HUMAN Activator [9]
Phospholipase D2 (PLD2) TTRLMKF PLD2_HUMAN Activator [10]
Voltage-gated potassium channel Kv7.2 (KCNQ2) TTPXI3S KCNQ2_HUMAN Activator [11]
Voltage-gated potassium channel Kv7.4 (KCNQ4) TT8HGRW KCNQ4_HUMAN Activator [11]

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: 2387).
2 Regulation of gating and rundown of HCN hyperpolarization-activated channels by exogenous and endogenous PIP2. J Gen Physiol. 2006 Nov;128(5):593-604.
3 Multiple PIP2 binding sites in Kir2.1 inwardly rectifying potassium channels. FEBS Lett. 2001 Feb 9;490(1-2):49-53.
4 Direct activation of inward rectifier potassium channels by PIP2 and its stabilization by Gbetagamma. Nature. 1998 Feb 19;391(6669):803-6.
5 Regulation of cardiac Na+,Ca2+ exchange and KATP potassium channels by PIP2. Science. 1996 Aug 16;273(5277):956-9.
6 PIP2 and PIP as determinants for ATP inhibition of KATP channels. Science. 1998 Nov 6;282(5391):1141-4.
7 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: 743).
8 Phosphatidylinositol 4,5-bisphosphate rescues TRPM4 channels from desensitization. J Biol Chem. 2005 Nov 25;280(47):39185-92.
9 The TRPM7 channel is inactivated by PIP(2) hydrolysis. Nat Cell Biol. 2002 May;4(5):329-36.
10 Cloning and initial characterization of a human phospholipase D2 (hPLD2). ADP-ribosylation factor regulates hPLD2. J Biol Chem. 1998 May 22;273(21):12846-52.
11 Regulation of Kv7 (KCNQ) K+ channel open probability by phosphatidylinositol 4,5-bisphosphate. J Neurosci. 2005 Oct 26;25(43):9825-35.
12 Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor. J Med Chem. 2010 Sep 23;53(18):6706-19.
13 LTRPC7 is a Mg.ATP-regulated divalent cation channel required for cell viability. Nature. 2001 May 31;411(6837):590-5.
14 Carvacrol is a novel inhibitor of Drosophila TRPL and mammalian TRPM7 channels. Cell Calcium. 2009 Mar;45(3):300-9.
15 Waixenicin A inhibits cell proliferation through magnesium-dependent block of transient receptor potential melastatin 7 (TRPM7) channels. J Biol Chem. 2011 Nov 11;286(45):39328-35.
16 Differential effects of general anesthetics on G protein-coupled inwardly rectifying and other potassium channels. Anesthesiology. 2001 Jul;95(1):144-53.
17 ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86.
18 Homomeric and heteromeric assembly of KCNQ (Kv7) K+ channels assayed by total internal reflection fluorescence/fluorescence resonance energy transfer and patch clamp analysis. J Biol Chem. 2008 Nov 7;283(45):30668-76.
19 Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants. Nat Chem Biol. 2007 May;3(5):287-96.
20 KCNQ4 channels expressed in mammalian cells: functional characteristics and pharmacology. Am J Physiol Cell Physiol. 2001 Apr;280(4):C859-66.
21 The acrylamide (S)-1 differentially affects Kv7 (KCNQ) potassium channels. Neuropharmacology. 2006 Nov;51(6):1068-77.
22 Identification of novel KCNQ4 openers by a high-throughput fluorescence-based thallium flux assay. Anal Biochem. 2011 Nov 1;418(1):66-72.
23 Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener. ACS Chem Neurosci. 2011 Oct 19;2(10):572-577.
24 Regulation of hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity by cCMP. J Biol Chem. 2012 Aug 3;287(32):26506-12.
25 Voltage-gated Potassium Channels as Therapeutic Drug Targets
26 Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol Pharmacol. 2000 Sep;58(3):591-600.
27 Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.
28 KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science. 1998 Dec 4;282(5395):1890-3.
29 Modulation of K(v)7 potassium channels by a novel opener pyrazolo[1,5-a]pyrimidin-7(4H)-one compound QO-58. Br J Pharmacol. 2013 Feb;168(4):1030-42.
30 The KCNQ2/3 selective channel opener ICA-27243 binds to a novel voltage-sensor domain site. Neurosci Lett. 2009 Nov 13;465(2):138-42.
31 Isoform-specific prolongation of Kv7 (KCNQ) potassium channel opening mediated by new molecular determinants for drug-channel interactions. J Biol Chem. 2010 Sep 3;285(36):28322-32.
32 Cytoplasmic accumulation of long-chain coenzyme A esters activates KATP and inhibits Kir2.1 channels. J Physiol. 2006 Sep 1;575(Pt 2):433-42.
33 Molecular basis for the inhibition of G protein-coupled inward rectifier K(+) channels by protein kinase C. Proc Natl Acad Sci U S A. 2004 Jan 27;101(4):1087-92.
34 Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b. Pflugers Arch. 2004 Apr;448(1):70-5.
35 Decavanadate modulates gating of TRPM4 cation channels. J Physiol. 2004 Nov 1;560(Pt 3):753-65.
36 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.
37 9-phenanthrol inhibits human TRPM4 but not TRPM5 cationic channels. Br J Pharmacol. 2008 Apr;153(8):1697-705.