Target family: Acid-sensing (proton-gated) ion channels (ASICs) (type: lgic)
Target: ASIC1

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Subunit-dependent high-affinity zinc inhibition of acid-sensing ion channels.
Published in: J Neurosci

Ligand: [125I]psalmotoxin 1 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKd
Reference (Journal): The receptor site of the spider toxin PcTx1 on the proton-gated cation channel ASIC1a.
Published in: J Physiol

Ligand: Pi-theraphotoxin-Hm3a (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Discovery and molecular interaction studies of a highly stable, tarantula peptide modulator of acid-sensing ion channel 1.
Published in: Neuropharmacology

Ligand: Pi-hexatoxin-Hi1a (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Experimental evidence that parasites drive eco-evolutionary feedbacks.
Published in: Proc Natl Acad Sci USA

Ligand: Pb2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Median affinity: 5.8 pIC50

Ligand: Pb2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Calcium-permeable acid-sensing ion channel is a molecular target of the neurotoxic metal ion lead.
Published in: J Biol Chem

Ligand: NS383 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 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: 4.900000095367432 pIC50
Reference (Journal): Nafamostat mesilate reversibly blocks acid-sensing ion channel currents.
Published in: Biochem Biophys Res Commun

Ligand: mambalgin-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Venom toxins in the exploration of molecular, physiological and pathophysiological functions of acid-sensing ion channels.
Published in: Toxicon

Ligand: mambalgin-1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Black mamba venom peptides target acid-sensing ion channels to abolish pain.
Published in: Nature

Ligand: JNJ-799760 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Molecular mechanism and structural basis of small-molecule modulation of the gating of acid-sensing ion channel 1.
Published in: Commun Biol

Ligand: JNJ-67869386 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Molecular mechanism and structural basis of small-molecule modulation of the gating of acid-sensing ion channel 1.
Published in: Commun Biol

Ligand: ibuprofen (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1974), EMA (2004)
Primary target: no
Median affinity: 3.5 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: ibuprofen (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1974), EMA (2004)
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen.
Published in: J Med Chem

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: flurbiprofen (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 3.5 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: ethylisopropylamiloride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): A proton-gated cation channel involved in acid-sensing.
Published in: Nature

Ligand: diminazene (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Molecular basis of inhibition of acid sensing ion channel 1A by diminazene.
Published in: PLoS One

Ligand: diminazene (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a).
Published in: Mol Pharmacol

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: compound 5b [PMID: 25974655] (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Novel Potent Orthosteric Antagonist of ASIC1a Prevents NMDAR-Dependent LTP Induction.
Published in: J Med Chem

Ligand: compound 5b [PMID: 25974655] (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): Novel Potent Orthosteric Antagonist of ASIC1a Prevents NMDAR-Dependent LTP Induction.
Published in: J Med Chem

Ligand: benzamil (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): A proton-gated cation channel involved in acid-sensing.
Published in: Nature

Ligand: ASC06-IgG1 (Antibody)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Selection of an ASIC1a-blocking combinatorial antibody that protects cells from ischemic death.
Published in: Proc Natl Acad Sci U S A

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 5 pIC50

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): A proton-gated cation channel involved in acid-sensing.
Published in: Nature

Ligand: A-317567 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels.
Published in: Pain