Target family: Transient Receptor Potential channels (TRP) (type: vgic)
Target: TRPM3

Ligand: 2-APB (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect.
Published in: Br J Pharmacol

Ligand: chloroform (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.7799999713897705 pIC50
Reference (Journal): Volatile anaesthetics inhibit the thermosensitive nociceptor ion channel transient receptor potential melastatin 3 (TRPM3).
Published in: Biochem Pharmacol

Ligand: CIM0216 (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.119999885559082 pEC50
Reference (Journal): Pharmacological properties of TRPM3 isoforms are determined by the length of the pore loop.
Published in: Br J Pharmacol

Ligand: CIM0216 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pEC50
Reference (Journal): Transient receptor potential TRPM3 channels: Pharmacology, signaling, and biological functions.
Published in: Pharmacol Res

Ligand: CIM0216 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pEC50
Reference (Journal): Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release.
Published in: Proc Natl Acad Sci USA

Ligand: clotrimazole (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: yes
Approval source: FDA (1975)
Primary target: no
Median affinity: 5.519999980926514 pEC50
Reference (Journal): Pharmacological properties of TRPM3 isoforms are determined by the length of the pore loop.
Published in: Br J Pharmacol

Ligand: diclofenac (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1988)
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Diclofenac, a nonsteroidal anti-inflammatory drug, is an antagonist of human TRPM3 isoforms.
Published in: Pharmacol Res Perspect

Ligand: dihydrosphingosine (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pEC50
Reference (Journal): Activation of the melastatin-related cation channel TRPM3 by D-erythro-sphingosine [corrected].
Published in: Mol Pharmacol

Ligand: epipregnanolone sulphate (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Cis-isomerism and other chemical requirements of steroidal agonists and partial agonists acting at TRPM3 channels.
Published in: Br J Pharmacol

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Molecular and functional characterization of the melastatin-related cation channel TRPM3.
Published in: J Biol Chem

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Expression and characterization of human transient receptor potential melastatin 3 (hTRPM3).
Published in: J Biol Chem

Ligand: halothane (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1958)
Primary target: no
Median affinity: 3.2799999713897705 pIC50
Reference (Journal): Volatile anaesthetics inhibit the thermosensitive nociceptor ion channel transient receptor potential melastatin 3 (TRPM3).
Published in: Biochem Pharmacol

Ligand: (S)-liquiritigenin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Flavanones that selectively inhibit TRPM3 attenuate thermal nociception in vivo.
Published in: Mol Pharmacol

Ligand: isosakuranetin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Flavanones that selectively inhibit TRPM3 attenuate thermal nociception in vivo.
Published in: Mol Pharmacol

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Molecular and functional characterization of the melastatin-related cation channel TRPM3.
Published in: J Biol Chem

Ligand: La3+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): Expression and characterization of human transient receptor potential melastatin 3 (hTRPM3).
Published in: J Biol Chem

Ligand: maprotiline (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1980)
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Primidone inhibits TRPM3 and attenuates thermal nociception in vivo.
Published in: Pain

Ligand: mefenamic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1967)
Primary target: no
Median affinity:  -
Reference (Journal): Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3.
Published in: Br J Pharmacol

Ligand: Mg2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 2 pIC50
Reference (Journal): Alternative splicing switches the divalent cation selectivity of TRPM3 channels.
Published in: J Biol Chem

Ligand: naringenin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Citrus fruit and fabacea secondary metabolites potently and selectively block TRPM3.
Published in: Br J Pharmacol

Ligand: naringenin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Flavanones that selectively inhibit TRPM3 attenuate thermal nociception in vivo.
Published in: Mol Pharmacol

Ligand: Na+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: nifedipine (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  -

Ligand: NN-dimethyl-D-erythrosphingosine (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Activation of the melastatin-related cation channel TRPM3 by D-erythro-sphingosine [corrected].
Published in: Mol Pharmacol

Ligand: pentafluoro-trityl clotrimazole analogue 29a (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Clotrimazole-Based Modulators of the TRPM3 Ion Channel Reveal Narrow Structure-Activity Relationship.
Published in: ACS Chem Biol

Ligand: pioglitazone (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: no
Median affinity:  -
Reference (Journal): Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels.
Published in: Mol Pharmacol

Ligand: pregnenolone sulphate (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Transient receptor potential M3 channels are ionotropic steroid receptors in pancreatic beta cells.
Published in: Nat Cell Biol

Ligand: primidone (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1954)
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Primidone inhibits TRPM3 and attenuates thermal nociception in vivo.
Published in: Pain

Ligand: rosiglitazone (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: no
Median affinity:  -
Reference (Journal): Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels.
Published in: Mol Pharmacol

Ligand: sphingosine (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.900000095367432 pEC50
Reference (Journal): Activation of the melastatin-related cation channel TRPM3 by D-erythro-sphingosine [corrected].
Published in: Mol Pharmacol

Ligand: troglitazone (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1997)
Primary target: no
Median affinity:  -