dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Interleukin-1 receptor-associated kinase (IRAK) family (type: enzyme)
Target: interleukin 1 receptor associated kinase 1

Ligand: belizatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pKd
Reference (Journal): The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Published in: J Med Chem

Ligand: compound 1 [WO2012007375] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pIC50
Reference (Patent): Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators.

Ligand: compound 7 [WO2012007375] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.010000228881836 pIC50
Reference (Patent): Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators.

Ligand: IRAK-1/4 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Published in: Bioorg Med Chem Lett

Ligand: Takinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.409999847412109 pIC50
Reference (Journal): Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease.
Published in: Cell Chem Biol
Target family: Interleukin-1 receptor-associated kinase (IRAK) family (type: enzyme)
Target: interleukin 1 receptor associated kinase 3

Ligand: compound R-16 [PMID: 21967808] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.
Published in: Bioorg Med Chem

Ligand: IRAK3 PROTAC 23 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.
Published in: J Med Chem
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.2

Ligand: Ba2+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Kir2.4: a novel K+ inward rectifier channel associated with motoneurons of cranial nerve nuclei.
Published in: J Neurosci
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.1

Ligand: spermine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): The tetravalent organic cation spermine causes the gating of the IRK1 channel expressed in murine fibroblast cells.
Published in: J Physiol (Lond.)

Ligand: spermine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKd
Reference (Journal): Control of rectification and permeation by residues in two distinct domains in an inward rectifier K+ channel.
Published in: Neuron
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>7.1

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pKi
Reference (Journal): Cloning and characterization of a novel human inwardly rectifying potassium channel predominantly expressed in small intestine.
Published in: FEBS Lett

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pKi
Reference (Journal): Functional Kir7.1 channels localized at the root of apical processes in rat retinal pigment epithelium.
Published in: J Physiol (Lond.)

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pKi
Reference (Journal): The epithelial inward rectifier channel Kir7.1 displays unusual K+ permeation properties.
Published in: J Neurosci

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.200000047683716 pKi
Reference (Journal): A novel inward rectifier K+ channel with unique pore properties.
Published in: Neuron
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>5.1

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Cloning and expression of a family of inward rectifier potassium channels.
Published in: Recept Channels

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): PSD-95 mediates formation of a functional homomeric Kir5.1 channel in the brain.
Published in: Neuron
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>4.2

Ligand: K+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Expression of a functional Kir4 family inward rectifier K+ channel from a gene cloned from mouse liver.
Published in: J Physiol (Lond.)

Ligand: K+ (Inorganic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Potassium-dependent activation of Kir4.2 K⁺ channels.
Published in: J Physiol (Lond.)

Ligand: H+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Differential pH sensitivity of Kir4.1 and Kir4.2 potassium channels and their modulation by heteropolymerisation with Kir5.1.
Published in: J Physiol (Lond.)

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Expression of a functional Kir4 family inward rectifier K+ channel from a gene cloned from mouse liver.
Published in: J Physiol (Lond.)

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Expression of a functional Kir4 family inward rectifier K+ channel from a gene cloned from mouse liver.
Published in: J Physiol (Lond.)
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>4.1

Ligand: VU0134992 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.010000228881836 pIC50
Reference (Journal): Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.
Published in: Mol Pharmacol

Ligand: nortriptyline (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1964)
Primary target: no
Median affinity:  pKd
Reference (Journal): Inhibition of astroglial inwardly rectifying Kir4.1 channels by a tricyclic antidepressant, nortriptyline.
Published in: J Pharmacol Exp Ther

Ligand: H+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Differential pH sensitivity of Kir4.1 and Kir4.2 potassium channels and their modulation by heteropolymerisation with Kir5.1.
Published in: J Physiol (Lond.)

Ligand: H+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): pH dependence of the inwardly rectifying potassium channel, Kir5.1, and localization in renal tubular epithelia.
Published in: J Biol Chem

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A novel ATP-dependent inward rectifier potassium channel expressed predominantly in glial cells.
Published in: J Biol Chem

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A novel ATP-dependent inward rectifier potassium channel expressed predominantly in glial cells.
Published in: J Biol Chem

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification of domains that control the heteromeric assembly of Kir5.1/Kir4.0 potassium channels.
Published in: Am J Physiol, Cell Physiol

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): In vivo formation of a proton-sensitive K+ channel by heteromeric subunit assembly of Kir5.1 with Kir4.1.
Published in: J Physiol (Lond.)
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>3.4

Ligand: tertiapin-Q (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): A novel high-affinity inhibitor for inward-rectifier K+ channels.
Published in: Biochemistry

Ligand: tertiapin-Q (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pIC50
Reference (Journal): Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q.
Published in: Biochemistry

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Regulation of cardiac Na+,Ca2+ exchange and KATP potassium channels by PIP2.
Published in: Science

Ligand: phorbol 12-myristate 13-acetate (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Median affinity:  -
Reference (Journal): Molecular basis for the inhibition of G protein-coupled inward rectifier K(+) channels by protein kinase C.
Published in: Proc Natl Acad Sci USA
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>7.1

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Median affinity:  -
Reference (Journal): A novel inward rectifier K+ channel with unique pore properties.
Published in: Neuron

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 1.600000023841858 pKi
Reference (Journal): The epithelial inward rectifier channel Kir7.1 displays unusual K+ permeation properties.
Published in: J Neurosci

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 1.600000023841858 pKi
Reference (Journal): A novel inward rectifier K+ channel with unique pore properties.
Published in: Neuron

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 1.600000023841858 pKi
Reference (Journal): Cloning and characterization of a novel human inwardly rectifying potassium channel predominantly expressed in small intestine.
Published in: FEBS Lett
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.3

Ligand: rose bengal (photoactivated) (Synthetic organic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Susceptibility of cloned K+ channels to reactive oxygen species.
Published in: Proc Natl Acad Sci USA

Ligand: SCH-23390 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Classic D1 dopamine receptor antagonist R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) directly inhibits G protein-coupled inwardly rectifying potassium channels.
Published in: Mol Pharmacol

Ligand: spermidine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Potassium channel block by cytoplasmic polyamines as the mechanism of intrinsic rectification.
Published in: Nature

Ligand: spermine (Metabolite)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Potassium channel block by cytoplasmic polyamines as the mechanism of intrinsic rectification.
Published in: Nature

Ligand: tenidap (Synthetic organic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3.
Published in: Eur J Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 4.21 pKi
Reference (Journal): Cloning and expression of a novel human brain inward rectifier potassium channel.
Published in: J Biol Chem

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification and molecular localization of a pH-sensing domain for the inward rectifier potassium channel HIR.
Published in: Neuron
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.4

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.319999933242798 pKd
Reference (Journal): Cloning and functional expression of human retinal kir2.4, a pH-sensitive inwardly rectifying K(+) channel.
Published in: Am J Physiol, Cell Physiol

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Functional expression of inward rectifier potassium channels in cultured human pulmonary smooth muscle cells: evidence for a major role of Kir2.4 subunits.
Published in: J Membr Biol
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>3.4

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): PIP2 and PIP as determinants for ATP inhibition of KATP channels.
Published in: Science
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.4

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Kir2.4: a novel K+ inward rectifier channel associated with motoneurons of cranial nerve nuclei.
Published in: J Neurosci

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Cloning and functional expression of human retinal kir2.4, a pH-sensitive inwardly rectifying K(+) channel.
Published in: Am J Physiol, Cell Physiol

Ligand: Cs+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 2.09 pKi
Reference (Journal): Kir2.4: a novel K+ inward rectifier channel associated with motoneurons of cranial nerve nuclei.
Published in: J Neurosci

Ligand: H+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Median affinity: 7.14 pKi
Reference (Journal): Cloning and functional expression of human retinal kir2.4, a pH-sensitive inwardly rectifying K(+) channel.
Published in: Am J Physiol, Cell Physiol

Ligand: Mg2+ (Inorganic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>3.1

Ligand: AZD2927 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: yes
Median affinity: 5.900000095367432 pIC50
Reference (Webpage): AZD2927.

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Atrial G protein-activated K+ channel: expression cloning and molecular properties.
Published in: Proc Natl Acad Sci USA

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Atrial G protein-activated K+ channel: expression cloning and molecular properties.
Published in: Proc Natl Acad Sci USA

Ligand: Ba2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Cloning of a G protein-activated inwardly rectifying potassium channel from human cerebellum.
Published in: Brain Res Mol Brain Res

Ligand: ethanol (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): G-protein-coupled inwardly rectifying potassium channels are targets of alcohol action.
Published in: Nat Neurosci

Ligand: ethanol (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Ethanol opens G-protein-activated inwardly rectifying K+ channels.
Published in: Nat Neurosci
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>3.1

Ligand: ML297 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice.
Published in: ACS Chem Neurosci

Ligand: Na+ (Inorganic)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular determinants for sodium-dependent activation of G protein-gated K+ channels.
Published in: J Biol Chem

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pKd
Reference (Journal): Direct activation of inward rectifier potassium channels by PIP2 and its stabilization by Gbetagamma.
Published in: Nature

Ligand: tertiapin-Q (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pIC50
Reference (Journal): Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q.
Published in: Biochemistry

Ligand: tertiapin-Q (Peptide)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pEC50
Reference (Journal): A novel high-affinity inhibitor for inward-rectifier K+ channels.
Published in: Biochemistry

Ligand: VU0810464 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.139999866485596 pEC50
Reference (Journal): Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.
Published in: ACS Chem Neurosci

Ligand: VU0810464 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.78000020980835 pEC50
Reference (Journal): Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.
Published in: ACS Chem Neurosci
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>3.3

Ligand: PIP2 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Regulation of cardiac Na+,Ca2+ exchange and KATP potassium channels by PIP2.
Published in: Science
Target family: Inwardly rectifying potassium channels (K<sub>IR</sub>) (type: vgic)
Target: K<sub>ir</sub>2.2

Ligand: Mg2+ (Inorganic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.960000038146973 pIC50
Reference (Journal): Competition between Mg2+ and spermine for a cloned IRK2 channel expressed in a human cell line.
Published in: J Physiol (Lond.)

Ligand: Cs+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Molecular cloning and functional expression of cDNA encoding a second class of inward rectifier potassium channels in the mouse brain.
Published in: J Biol Chem

Ligand: Ba2+ (Inorganic)
Interaction type: Gating inhibitor
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Molecular cloning and functional expression of cDNA encoding a second class of inward rectifier potassium channels in the mouse brain.
Published in: J Biol Chem
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluN2A

Ligand: amantadine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1966)
Primary target: yes
Median affinity:  -