dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Type X RTKs: HGF (hepatocyte growth factor) receptor family (type: catalytic_receptor)
Target: macrophage stimulating 1 receptor

Ligand: BMS-777607 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.739999771118164 pIC50
Reference (Journal): Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
Published in: J Med Chem

Ligand: compound 19a [PMID: 30503936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Discovery of N<sup>1</sup>-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N<sup>3</sup>-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment.
Published in: Eur J Med Chem

Ligand: compound 8i [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.909999847412109 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: macrophage stimulating protein 1 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Type XVII RTKs: ROS receptors (type: catalytic_receptor)
Target: c-ros oncogene 1, receptor tyrosine kinase

Ligand: compound 8e [PMID: 24432909] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.699999809265137 pKi
Reference (Journal): Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Published in: J Med Chem

Ligand: gilteritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 8.819999694824219 pIC50
Reference (Journal): Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor.
Published in: Blood

Ligand: lorlatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: yes
Median affinity: 11.300000190734863 pKi
Reference (Journal): Abstract A277: PF-06463922, a novel ROS1/ALK inhibitor, demonstrates sub-nanomolar potency against oncogenic ROS1 fusions and capable of blocking the resistant ROS1G2032R mutant in preclinical tumor models.
Published in: Mol Cancer Ther

Ligand: repotrectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 10.149999618530273 pIC50
Reference (Journal): Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations.
Published in: Cancer Discov

Ligand: taletrectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models.
Published in: Nat Commun

Ligand: zidesamtinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations.
Published in: Cancer Discov

Ligand: zidesamtinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Patent): Heteroaromatic macrocyclic ether chemotherapeutic agents
Target family: UDP glucuronosyltransferases (UGT) (type: enzyme)
Target: UDP glucuronosyltransferase family 1 member A1

Ligand: ritonavir (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1996)
Primary target: no
Median affinity: 5.769999980926514 pIC50
Reference (Journal): Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
Published in: Drug Metab Dispos
Target family: Unc-51-like kinase (ULK) family (type: enzyme)
Target: unc-51 like autophagy activating kinase 2

Ligand: SBP-7455 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.940000057220459 pIC50
Reference (Journal): Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Published in: J Med Chem
Target family: Unc-51-like kinase (ULK) family (type: enzyme)
Target: unc-51 like autophagy activating kinase 1

Ligand: SBP-7455 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.
Published in: J Med Chem

Ligand: SBI-0206965 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates.
Published in: Mol Cell

Ligand: inlexisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Phenylaminopyrimidine amide autophagy inhibitors and methods of use thereof
Target family: Unc-51-like kinase (ULK) family (type: enzyme)
Target: serine/threonine kinase 36

Ligand: Ro-0505124 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.
Published in: J Biol Chem
Target family: Unc-51-like kinase (ULK) family (type: enzyme)
Target: unc-51 like autophagy activating kinase 1

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
Target family: Unc-51-like kinase (ULK) family (type: enzyme)
Target: unc-51 like kinase 3

Ligand: compound 15 [PMID: 24900237] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
Published in: ACS Med Chem Lett
Target family: Urate transporter (type: transporter)
Target: Urate anion exchanger 1

Ligand: verinurad (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: sufinpyrazone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 4 pIC50
Reference (Journal): Morin (3,5,7,2',4'-pentahydroxyflavone) exhibits potent inhibitory actions on urate transport by the human urate anion transporter (hURAT1) expressed in human embryonic kidney cells.
Published in: Drug Metab Dispos

Ligand: lesinurad (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity:  -
Reference (Journal): Gout therapeutics: new drugs for an old disease.
Published in: Lancet

Ligand: dotinurad (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2018)
Primary target: yes
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Pharmacological Evaluation of Dotinurad, a Selective Urate Reabsorption Inhibitor.
Published in: J Pharmacol Exp Ther
Target family: Vasopressin and oxytocin receptors (type: gpcr)
Target: V<sub>1A</sub> receptor

Ligand: [3H]d(CH2)5[Tyr(Me)2]AVP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKd
Target family: Vesicular nucleotide transporter (type: transporter)
Target: Vesicular nucleotide transporter

Ligand: clodronic acid (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: UK (1999)
Primary target: no
Median affinity: 7.809999942779541 pIC50
Reference (Journal): Identification of a vesicular ATP release inhibitor for the treatment of neuropathic and inflammatory pain.
Published in: Proc Natl Acad Sci USA
Target family: Voltage-gated calcium channels  (Ca<sub>V</sub>) (type: vgic)
Target: Ca<sub>v</sub>1.3

Ligand: isradipine (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: yes
Approval source: FDA (1990)
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>2.2

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: yes
Median affinity: 2.799999952316284 pIC50
Reference (Journal): Molecular identification of a component of delayed rectifier current in gastrointestinal smooth muscles.
Published in: Am J Physiol

Ligand: GxTx-1E (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Journal): Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion.
Published in: Diabetes

Ligand: quinine (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2005, as quinine sulfate, previous history unspecified)
Median affinity: 4.9 pIC50
Reference (Journal): Molecular identification of a component of delayed rectifier current in gastrointestinal smooth muscles.
Published in: Am J Physiol

Ligand: RY785 (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Identification of novel and selective Kv2 channel inhibitors.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.3

Ligand: encukalner (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Derivatives of 4-(n-azacycloalkyl) anilides as potassium channel modulators

Ligand: gabapentin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 8.279999732971191 pEC50
Reference (Journal): Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels.
Published in: Mol Pharmacol

Ligand: linopirdine (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel.
Published in: Science

Ligand: retigabine (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA and EMA (2011)
Primary target: yes
Median affinity: 6.199999809265137 pEC50
Reference (Journal): Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine.
Published in: J Neurosci

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 1.5 pIC50
Reference (Journal): Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels.
Published in: Br J Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.5

Ligand: flindokalner (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.
Published in: Eur J Pharmacol

Ligand: gabapentin (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 8.720000267028809 pEC50
Reference (Journal): Gabapentin Is a Potent Activator of KCNQ3 and KCNQ5 Potassium Channels.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>2.2

Ligand: RY796 (Synthetic organic)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Identification of novel and selective Kv2 channel inhibitors.
Published in: Mol Pharmacol

Ligand: ScTx1 (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Novel tarantula toxins for subtypes of voltage-dependent potassium channels in the Kv2 and Kv4 subfamilies.
Published in: Mol Pharmacol

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 2.5999999046325684 pIC50
Reference (Journal): Molecular identification of a component of delayed rectifier current in gastrointestinal smooth muscles.
Published in: Am J Physiol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>3.2

Ligand: fampridine (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (2010), EMA (2011)
Primary target: no
Median affinity: 4.599999904632568 pIC50
Reference (Journal): Gating, modulation and subunit composition of voltage-gated K(+) channels in dendritic inhibitory interneurones of rat hippocampus.
Published in: J Physiol (Lond.)
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.1

Ligand: azimilide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Journal): The role of the IsK protein in the specific pharmacological properties of the IKs channel complex.
Published in: Br J Pharmacol

Ligand: 3S,4R-293B (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.519999980926514 pIC50
Reference (Journal): A kinetic study on the stereospecific inhibition of KCNQ1 and I(Ks) by the chromanol 293B.
Published in: Br J Pharmacol

Ligand: (3R,4S)-293B (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A kinetic study on the stereospecific inhibition of KCNQ1 and I(Ks) by the chromanol 293B.
Published in: Br J Pharmacol

Ligand: (3R,4S)-293B (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Characterization of recombinant human cardiac KCNQ1/KCNE1 channels (I (Ks)) stably expressed in HEK 293 cells.
Published in: J Membr Biol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>4.1

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2 pIC50
Reference (Journal): Endogenous Kv channels in human embryonic kidney (HEK-293) cells.
Published in: Mol Cell Biochem
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.5

Ligand: linopirdine (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pKd
Reference (Journal): Molecular cloning and functional expression of KCNQ5, a potassium channel subunit that may contribute to neuronal M-current diversity.
Published in: J Biol Chem

Ligand: retigabine (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA and EMA (2011)
Primary target: yes
Median affinity: 5 pEC50
Reference (Journal): Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.
Published in: Eur J Pharmacol

Ligand: retigabine derivative 10g (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Discovery of Novel Retigabine Derivatives as Potent KCNQ4 and KCNQ5 Channel Agonists with Improved Specificity.
Published in: ACS Med Chem Lett

Ligand: (S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Reference (Journal): The acrylamide (S)-1 differentially affects Kv7 (KCNQ) potassium channels.
Published in: Neuropharmacology

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): KCNQ5, a novel potassium channel broadly expressed in brain, mediates M-type currents.
Published in: J Biol Chem

Ligand: tetraethylammonium (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning and functional expression of KCNQ5, a potassium channel subunit that may contribute to neuronal M-current diversity.
Published in: J Biol Chem

Ligand: XE991 (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): KCNQ5, a novel potassium channel broadly expressed in brain, mediates M-type currents.
Published in: J Biol Chem

Ligand: zinc pyrithione (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants.
Published in: Nat Chem Biol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>2.1

Ligand: halothane (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1958)
Median affinity: 3.5 pEC50
Reference (Journal): Inhibitory effects of ketamine and halothane on recombinant potassium channels from mammalian brain.
Published in: Anesthesiology

Ligand: jingzhaotoxin-III (Peptide)
Interaction type: Gating inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Solution structure of Jingzhaotoxin-III, a peptide toxin inhibiting both Nav1.5 and Kv2.1 channels.
Published in: Toxicon
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.2

Ligand: encukalner (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Derivatives of 4-(n-azacycloalkyl) anilides as potassium channel modulators

Ligand: flindokalner (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): KCNQ4 channel activation by BMS-204352 and retigabine.
Published in: Neuropharmacology
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>10.2

Ligand: LY97241 (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents.
Published in: Mol Pharmacol

Ligand: LY97241 (Synthetic organic)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Carboxy-terminal domain mediates assembly of the voltage-gated rat ether-à-go-go potassium channel.
Published in: EMBO J

Ligand: quinidine (Natural product)
Interaction type: Channel blocker
Action: Pore blocker
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity: 3.799999952316284 pIC50
Reference (Journal): Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>1.1

Ligand: α-dendrotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol

Ligand: α-dendrotoxin (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of amino acid residues involved in dendrotoxin block of rat voltage-dependent potassium channels.
Published in: Mol Pharmacol

Ligand: capsaicin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: no
Median affinity: 4.5 pIC50
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol

Ligand: dendrotoxin-I (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
Published in: Mol Pharmacol
Target family: Voltage-gated potassium channels (K<sub>v</sub>) (type: vgic)
Target: K<SUB>v</SUB>7.1

Ligand: HMR-1556 (Synthetic organic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Characterization of recombinant human cardiac KCNQ1/KCNE1 channels (I (Ks)) stably expressed in HEK 293 cells.
Published in: J Membr Biol