Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPM4

Ligand: 9-phenanthrol (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): 9-phenanthrol inhibits human TRPM4 but not TRPM5 cationic channels.
Published in: Br J Pharmacol

Ligand: adenosine (Metabolite)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 3.200000047683716 pIC50

Ligand: adenosine 5'-monophosphate (Metabolite)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 4.7 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch

Ligand: ADP (Metabolite)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch

Ligand: AMP-PNP (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 4.7 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch

Ligand: ATP (Metabolite)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 4.9 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch

Ligand: ATP (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch

Ligand: ATP (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pIC50
Reference (Journal): Comparison of functional properties of the Ca2+-activated cation channels TRPM4 and TRPM5 from mice.
Published in: Cell Calcium

Ligand: BTP2 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pEC50
Reference (Journal): A pyrazole derivative potently inhibits lymphocyte Ca2+ influx and cytokine production by facilitating transient receptor potential melastatin 4 channel activity.
Published in: Mol Pharmacol

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Regulation of the Ca2+ sensitivity of the nonselective cation channel TRPM4.
Published in: J Biol Chem

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A pyrazole derivative potently inhibits lymphocyte Ca2+ influx and cytokine production by facilitating transient receptor potential melastatin 4 channel activity.
Published in: Mol Pharmacol

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The Ca2+-activated cation channel TRPM4 is regulated by phosphatidylinositol 4,5-biphosphate.
Published in: EMBO J

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Decavanadate modulates gating of TRPM4 cation channels.
Published in: J Physiol (Lond.)

Ligand: clotrimazole (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity:  -
Reference (Book): PhD Thesis.
Published in: TRPM4 and TRPM5: Functional characterisation and comparison of two novel Ca<sup>2+</sup>-activated cation channels of the TRPM subfamily

Ligand: compound 5 [PMID: 29579323] (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pIC50
Reference (Journal): Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Published in: Br J Pharmacol

Ligand: compound 5 [PMID: 29579323] (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pIC50
Reference (Journal): Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Published in: Br J Pharmacol

Ligand: compound 6 [PMID: 29579323] (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Identification of potent and selective small molecule inhibitors of the cation channel TRPM4.
Published in: Br J Pharmacol

Ligand: compound 6 [PMID: 29579323] (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Investigation of Novel Small Molecular TRPM4 Inhibitors in Colorectal Cancer Cells.
Published in: Cancers (Basel)

Ligand: decavanadate (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pEC50
Reference (Journal): Decavanadate modulates gating of TRPM4 cation channels.
Published in: J Physiol (Lond.)

Ligand: flufenamic acid (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 5.599999904632568 pIC50
Reference (Journal): Comparison of functional properties of the Ca2+-activated cation channels TRPM4 and TRPM5 from mice.
Published in: Cell Calcium

Ligand: LBA (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Investigation of Novel Small Molecular TRPM4 Inhibitors in Colorectal Cancer Cells.
Published in: Cancers (Basel)

Ligand: meclofenamic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Primary target: no
Median affinity: 5.46999979019165 pIC50
Reference (Journal): TRPM4 inhibition by meclofenamate suppresses Ca2+-dependent triggered arrhythmias.
Published in: Eur Heart J

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): The Ca2+-activated cation channel TRPM4 is regulated by phosphatidylinositol 4,5-biphosphate.
Published in: EMBO J

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity: 5.2 pEC50
Reference (Journal): Phosphatidylinositol 4,5-bisphosphate rescues TRPM4 channels from desensitization.
Published in: J Biol Chem

Ligand: spermine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 4.5 pIC50
Reference (Journal): Comparison of functional properties of the Ca2+-activated cation channels TRPM4 and TRPM5 from mice.
Published in: Cell Calcium

Ligand: spermine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): Intracellular nucleotides and polyamines inhibit the Ca2+-activated cation channel TRPM4b.
Published in: Pflugers Arch