dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &delta; subunit

Ligand: DS2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev

Ligand: gaboxadol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: tracazolate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): International Union of Basic and Clinical Pharmacology. CVI: GABA<sub>A</sub> Receptor Subtype- and Function-selective Ligands: Key Issues in Translation to Humans.
Published in: Pharmacol Rev
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &epsilon; subunit

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &gamma;1 subunit

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &alpha;5 subunit

Ligand: triazolam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1982)
Primary target: yes
Median affinity: 8.8100004196167 pKi
Reference (Journal): Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
Published in: J Med Chem
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &gamma;2 subunit

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &rho;3 subunit

Ligand: aza-THIP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: 5-Me-IAA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &rho;2 subunit

Ligand: TPMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: (±)-cis-2-CAMP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: piperidine-4-sulphonic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: muscimol (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: trans-3-ACPBPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isonipecotic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isoguvacine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: cis-3-ACPBPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: gaboxadol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Aza-THIP and related analogues of THIP as GABA C antagonists.
Published in: Bioorg Med Chem

Ligand: aza-THIP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: 5-Me-IAA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &rho;1 subunit

Ligand: TPMPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: (±)-cis-2-CAMP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: piperidine-4-sulphonic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: muscimol (Natural product)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: trans-3-ACPBPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isonipecotic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: isoguvacine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: cis-3-ACPBPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: gaboxadol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Aza-THIP and related analogues of THIP as GABA C antagonists.
Published in: Bioorg Med Chem

Ligand: CACA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.130000114440918 pEC50
Reference (Journal): Characterization of bicuculline/baclofen-insensitive (rho-like) gamma-aminobutyric acid receptors expressed in Xenopus oocytes. II. Pharmacology of gamma-aminobutyric acidA and gamma-aminobutyric acidB receptor agonists and antagonists.
Published in: Mol Pharmacol

Ligand: aza-THIP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -

Ligand: 5-Me-IAA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>A</sub> receptors (type: lgic)
Target: GABA<sub>A</sub> receptor &pi; subunit

Ligand: TBPS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA<sub>B</sub> receptors (type: gpcr)
Target: GABA<sub>B1</sub>

Ligand: saclofen (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
Published in: Nature
Target family: GABA<sub>B</sub> receptors (type: gpcr)
Target: GABA<sub>B</sub> receptor

Ligand: [3H](R)-(-)-baclofen (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]CGP 62349 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Characterisation and partial purification of the GABA(B) receptor from the rat cerebellum using the novel antagonist [3H]CGP 62349.
Published in: Brain Res Mol Brain Res
Target family: GABA<sub>B</sub> receptors (type: gpcr)
Target: GABA<sub>B2</sub>

Ligand: CGP7930 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor.
Published in: J Biol Chem

Ligand: CGP7930 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.7 pEC50
Reference (Journal): Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501.
Published in: Mol Pharmacol
Target family: GABA<sub>B</sub> receptors (type: gpcr)
Target: GABA<sub>B1</sub>

Ligand: [125I]CGP 71872 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
Published in: Nature

Ligand: [125I]CGP 64213 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors.
Published in: Nature

Ligand: SCH 50911 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): The pharmacology of SCH 50911: a novel, orally-active GABA-beta receptor antagonist.
Published in: J Pharmacol Exp Ther
Target family: GABA transporter subfamily (type: transporter)
Target: GAT1

Ligand: NNC-711 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Tiagabine, SK&amp;F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.
Published in: Eur J Pharmacol

Ligand: CI-966 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Tiagabine, SK&amp;F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.
Published in: Eur J Pharmacol
Target family: GABA transporter subfamily (type: transporter)
Target: BGT1

Ligand: (S)-EF-1520 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: (R/S) EF-1500 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 4.9 pIC50

Ligand: (R)-EF-1520 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: NNC052090 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): 1-(3-(9H-carbazol-9-yl)-1-propyl)-4-(2-methoxyphenyl)-4-piperidinol, a novel subtype selective inhibitor of the mouse type II GABA-transporter.
Published in: Br J Pharmacol

Ligand: LU32-176B (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.
Published in: J Pharmacol Exp Ther
Target family: GABA transporter subfamily (type: transporter)
Target: GAT1

Ligand: (R)-EF-1520 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: LU32-176B (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.
Published in: J Pharmacol Exp Ther
Target family: GABA transporter subfamily (type: transporter)
Target: GAT3

Ligand: SNAP-5114 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.179999828338623 pIC50
Reference (Journal): Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site.
Published in: Recept Channels
Target family: GABA transporter subfamily (type: transporter)
Target: GAT2

Ligand: SNAP-5114 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site.
Published in: Recept Channels
Target family: GABA transporter subfamily (type: transporter)
Target: GAT1

Ligand: tiagabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Tiagabine, SK&amp;F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.
Published in: Eur J Pharmacol

Ligand: [3H]tiagabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -

Ligand: SKF89976A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 pIC50
Reference (Journal): On the bioactive conformation of the GABA uptake inhibitor SK&amp;F 89976-A.
Published in: Bioorg Med Chem Lett

Ligand: (S)-EF-1520 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50

Ligand: (R/S) EF-1500 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Target family: GABA turnover (type: enzyme)
Target: 4-aminobutyrate aminotransferase

Ligand: vigabatrin (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: yes
Approval source: FDA (2009), EMA (2018)
Primary target: yes
Median affinity: 3.069999933242798 pKi
Reference (Journal): The 2011 E. B. Hershberg award for important discoveries in medicinally active substances: (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA aminotransferase inactivator and new treatment for drug addiction and infantile spasms.
Published in: J Med Chem

Ligand: CPP-115 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.010000228881836 pKi
Reference (Journal): The 2011 E. B. Hershberg award for important discoveries in medicinally active substances: (1S,3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a GABA aminotransferase inactivator and new treatment for drug addiction and infantile spasms.
Published in: J Med Chem

Ligand: 4-acryloylphenol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.260000228881836 pIC50
Reference (Journal): Inhibition of GABA shunt enzymes' activity by 4-hydroxybenzaldehyde derivatives.
Published in: Bioorg Med Chem Lett
Target family: GABA turnover (type: enzyme)
Target: aldehyde dehydrogenase 5 family member A1

Ligand: 4-acryloylphenol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.460000038146973 pIC50
Reference (Journal): Inhibition of GABA shunt enzymes' activity by 4-hydroxybenzaldehyde derivatives.
Published in: Bioorg Med Chem Lett
Target family: GABA turnover (type: enzyme)
Target: Glutamic acid decarboxylase 2

Ligand: s-allylglycine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA turnover (type: enzyme)
Target: Glutamic acid decarboxylase 1

Ligand: s-allylglycine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: GABA turnover (type: enzyme)
Target: 4-aminobutyrate aminotransferase

Ligand: vigabatrin (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: yes
Approval source: FDA (2009), EMA (2018)
Primary target: yes
Median affinity: 3.069999933242798 pKi
Reference (Journal): 4-amino-hex-5-enoic acid, a selective catalytic inhibitor of 4-aminobutyric-acid aminotransferase in mammalian brain.
Published in: Eur J Biochem
Target family: G-alpha family G(q) subfamily (type: enzyme)
Target: G protein subunit alpha q

Ligand: YM-254890 (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.019999980926514 pIC50
Reference (Webpage): Total synthesis and structure activity relationship studies of a series of selective G protein inhibitors

Ligand: FR900359 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.480000019073486 pIC50
Reference (Webpage): Total synthesis and structure activity relationship studies of a series of selective G protein inhibitors
Target family: Gasdermins (GSDM) (type: other_protein)
Target: gasdermin D

Ligand: LDC7559 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Gasdermin D (GSDMD) as a new target for the treatment of infection.
Published in: Medchemcomm

Ligand: disulfiram (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1951)
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Gasdermin D (GSDMD) as a new target for the treatment of infection.
Published in: Medchemcomm
Target family: GCN2 subfamily (type: enzyme)
Target: eukaryotic translation initiation factor 2 alpha kinase 4

Ligand: compound A127 [WO2013110309] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2.
Published in: ACS Med Chem Lett

Ligand: compound 39 [PMID: 36127295] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.
Published in: J Med Chem

Ligand: HC-7366 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.
Published in: J Med Chem
Target family: GDNF receptor family (type: catalytic_receptor)
Target: GDNF family receptor &alpha;1

Ligand: [125I]GDNF (rat) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  pKd
Reference (Journal): A GPI-linked protein that interacts with Ret to form a candidate neurturin receptor.
Published in: Nature
Target family: GDNF receptor family (type: catalytic_receptor)
Target: GDNF family receptor alpha like

Ligand: LY3463251 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pEC50
Reference (Journal): Discovery, development, and clinical proof of mechanism of LY3463251, a long-acting GDF15 receptor agonist.
Published in: Cell Metab

Ligand: LY3463251 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.869999885559082 pEC50
Reference (Journal): Discovery, development, and clinical proof of mechanism of LY3463251, a long-acting GDF15 receptor agonist.
Published in: Cell Metab

Ligand: LY3463251 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pKd
Reference (Journal): Discovery, development, and clinical proof of mechanism of LY3463251, a long-acting GDF15 receptor agonist.
Published in: Cell Metab

Ligand: growth differentiation factor 15 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKd
Reference (Journal): The metabolic effects of GDF15 are mediated by the orphan receptor GFRAL.
Published in: Nat Med

Ligand: GRASP (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pKd
Reference (Journal): Creation of a Peptide Antagonist of the GFRAL-RET Receptor Complex for the Treatment of GDF15-Induced Malaise.
Published in: J Med Chem
Target family: GDNF receptor family (type: catalytic_receptor)
Target: GDNF family receptor &alpha;1

Ligand: [125I]GDNF (rat) (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of a multicomponent receptor for GDNF.
Published in: Nature
Target family: GEK subfamily (type: enzyme)
Target: DM1 protein kinase

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.46999979019165 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm
Target family: GEK subfamily (type: enzyme)
Target: CDC42 binding protein kinase beta

Ligand: A-443654 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Inhibitor hijacking of Akt activation.
Published in: Nat Chem Biol
Target family: GEK subfamily (type: enzyme)
Target: CDC42 binding protein kinase alpha

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm

Ligand: compound 11d [DOI: 10.1039/c0md00194e] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors.
Published in: Medchemcomm