Target family: Acid-sensing (proton-gated) ion channels (ASICs) (type: lgic)
Target: ASIC3

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): Inhibitory regulation of acid-sensing ion channel 3 by zinc.
Published in: Neuroscience

Ligand: Ugr 9-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Sea anemone peptide with uncommon β-hairpin structure inhibits acid-sensing ion channel 3 (ASIC3) and reveals analgesic activity.
Published in: J Biol Chem

Ligand: salicylic acid (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Primary target: no
Median affinity: 3.5999999046325684 pIC50
Reference (Journal): Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors.
Published in: J Neurosci

Ligand: NS383 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): NS383 Selectively Inhibits Acid-Sensing Ion Channels Containing 1a and 3 Subunits to Reverse Inflammatory and Neuropathic Hyperalgesia in Rats.
Published in: CNS Neurosci Ther

Ligand: nafamostat (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: Japan only
Primary target: no
Median affinity: 5.599999904632568 pIC50
Reference (Journal): Nafamostat mesilate reversibly blocks acid-sensing ion channel currents.
Published in: Biochem Biophys Res Commun

Ligand: lysophosphatidylcholine (Metabolite)
Interaction type: Activator
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pEC50
Reference (Journal): Non-acidic activation of pain-related Acid-Sensing Ion Channel 3 by lipids.
Published in: EMBO J

Ligand: H+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  pEC50

Ligand: H+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  pEC50

Ligand: GMQ (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 3 pEC50
Reference (Journal): A nonproton ligand sensor in the acid-sensing ion channel.
Published in: Neuron

Ligand: Gd3+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.400000095367432 pIC50
Reference (Journal): Mammalian ASIC2a and ASIC3 subunits co-assemble into heteromeric proton-gated channels sensitive to Gd3+.
Published in: J Biol Chem

Ligand: diminazene (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain.
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: 4 pIC50
Reference (Journal): Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors.
Published in: J Neurosci

Ligand: aspirin (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (no history prior to 1965)
Median affinity: 4 pIC50
Reference (Journal): Nonsteroid anti-inflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors.
Published in: J Neurosci

Ligand: arcaine (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2.9000000953674316 pEC50
Reference (Journal): ASIC3 channels integrate agmatine and multiple inflammatory signals through the nonproton ligand sensing domain.
Published in: Mol Pain

Ligand: APETx2 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): A new sea anemone peptide, APETx2, inhibits ASIC3, a major acid-sensitive channel in sensory neurons.
Published in: EMBO J

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning of a non-inactivating proton-gated Na+ channel specific for sensory neurons.
Published in: J Biol Chem

Ligand: agmatine (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2 pEC50
Reference (Journal): ASIC3 channels integrate agmatine and multiple inflammatory signals through the nonproton ligand sensing domain.
Published in: Mol Pain

Ligand: A-317567 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.989999771118164 pIC50
Reference (Journal): Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567.
Published in: ACS Chem Neurosci