dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluK3

Ligand: domoic acid (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.420000076293945 pKi
Reference (Journal): Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Published in: J Med Chem

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

Ligand: kainate (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pKi
Reference (Journal): Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Published in: J Med Chem

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

Ligand: [3H]SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]UBP310 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pKd
Reference (Journal): Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310.
Published in: Mol Pharmacol

Ligand: SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pKi
Reference (Journal): Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Published in: J Med Chem
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluK4

Ligand: domoic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

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

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

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

Ligand: [3H]SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluK5

Ligand: domoic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

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

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

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

Ligand: [3H]SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: SYM2081 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluN2A

Ligand: 5,7-dichlorokynurenic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Primary target: no
Median affinity:  -
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluA1

Ligand: aniracetam (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Primary target: no
Median affinity:  -
Target family: Ionotropic glutamate receptors (type: lgic)
Target: GluA1

Ligand: AMPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Iota subfamily (type: enzyme)
Target: protein kinase C zeta

Ligand: Gö 6983 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes.
Published in: FEBS Lett

Ligand: compound 3 [PMID: 19097791] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.649999618530273 pIC50
Reference (Journal): 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: balanol (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.230000019073486 pIC50
Reference (Journal): Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Published in: J Med Chem

Ligand: arachidonic acid (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  -
Reference (Journal): PKC zeta is a molecular switch in signal transduction of TNF-alpha, bifunctionally regulated by ceramide and arachidonic acid.
Published in: EMBO J
Target family: Iota subfamily (type: enzyme)
Target: protein kinase C iota

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.460000038146973 pIC50
Reference (Journal): Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.
Published in: J Biol Chem
Target family: IP<sub>3</sub> receptors (type: lgic)
Target: IP<sub>3</sub>R1

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Median affinity:  -

Ligand: adenophostin A (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: ATP (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Target family: IP<sub>3</sub> receptors (type: lgic)
Target: IP<sub>3</sub>R3

Ligand: IP3 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: decavanadate (Inorganic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Target family: IP<sub>3</sub> receptors (type: lgic)
Target: IP<sub>3</sub>R2

Ligand: IP3 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: inositol 2,4,5-trisphosphate (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: decavanadate (Inorganic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: adenophostin A (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Target family: IP<sub>3</sub> receptors (type: lgic)
Target: IP<sub>3</sub>R1

Ligand: xestospongin C (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: PIP2 (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: IP3 (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: inositol 2,4,5-trisphosphate (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -

Ligand: decavanadate (Inorganic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -

Ligand: Ca2+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Target family: IRE family (type: enzyme)
Target: endoplasmic reticulum to nucleus signaling 1

Ligand: compound 34 [PMID: 24749861] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pIC50
Reference (Journal): Synthesis of novel tricyclic chromenone-based inhibitors of IRE-1 RNase activity.
Published in: J Med Chem
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase

Ligand: fosmidomycin (Natural product)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.539999961853027 pIC50
Reference (Journal): Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs.
Published in: Science
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase

Ligand: MMV008138 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): A chemical rescue screen identifies a Plasmodium falciparum apicoplast inhibitor targeting MEP isoprenoid precursor biosynthesis.
Published in: Antimicrob Agents Chemother
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase

Ligand: AIM-1290 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
Published in: Bioorg Med Chem Lett

Ligand: AIM-1290 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.710000038146973 pIC50
Reference (Journal): Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
Published in: Bioorg Med Chem Lett

Ligand: MMV019313 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.570000171661377 pEC50
Reference (Journal): Specific Inhibition of the Bifunctional Farnesyl/Geranylgeranyl Diphosphate Synthase in Malaria Parasites via a New Small-Molecule Binding Site.
Published in: Cell Chem Biol

Ligand: MMV019313 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.739999771118164 pEC50
Reference (Journal): Specific Inhibition of the Bifunctional Farnesyl/Geranylgeranyl Diphosphate Synthase in Malaria Parasites via a New Small-Molecule Binding Site.
Published in: Cell Chem Biol
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase

Ligand: fosmidomycin (Natural product)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.429999828338623 pIC50
Reference (Journal): Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs.
Published in: Science
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum 2-C-methyl-D-erythritol 4-phosphate cytidylyltransferase

Ligand: MMV008138 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.960000038146973 pEC50
Reference (Journal): A chemical rescue screen identifies a Plasmodium falciparum apicoplast inhibitor targeting MEP isoprenoid precursor biosynthesis.
Published in: Antimicrob Agents Chemother

Ligand: MMV008138 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies.
Published in: Bioorg Med Chem Lett
Target family: Isoprenoid biosynthesis enzymes  (type: other_protein)
Target: Plasmodium falciparum 1-deoxy-D-xylulose 5-phosphate reductoisomerase

Ligand: fosmidomycin (Natural product)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.460000038146973 pIC50
Reference (Journal): Inhibitors of the nonmevalonate pathway of isoprenoid biosynthesis as antimalarial drugs.
Published in: Science
Target family: Janus kinase (JakA) family (type: enzyme)
Target: Janus kinase 2

Ligand: compound 13 [PMID: 35653642] (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pKd
Reference (Journal): Insights on JAK2 Modulation by Potent, Selective, and Cell-Permeable Pseudokinase-Domain Ligands.
Published in: J Med Chem
Target family: KHS subfamily (type: enzyme)
Target: mitogen-activated protein kinase kinase kinase kinase 1

Ligand: compound 5i [PMID: 36542759] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Published in: J Med Chem
Target family: KHS subfamily (type: enzyme)
Target: mitogen-activated protein kinase kinase kinase kinase 2

Ligand: BAY 61-3606 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.949999809265137 pIC50
Reference (Journal): BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner.
Published in: PLoS ONE

Ligand: belizatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 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: NG-25 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2).
Published in: J Med Chem
Target family: KHS subfamily (type: enzyme)
Target: mitogen-activated protein kinase kinase kinase kinase 3

Ligand: compound 5i [PMID: 36542759] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.090000152587891 pIC50
Reference (Journal): Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy.
Published in: J Med Chem

Ligand: compound 8h [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: RIPK3 inhibitor 18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
Published in: ACS Med Chem Lett
Target family: KHS subfamily (type: enzyme)
Target: mitogen-activated protein kinase kinase kinase kinase 5

Ligand: bosutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Published in: Leukemia

Ligand: NIK SMI1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
Reference (Journal): NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Published in: Nat Commun

Ligand: RIPK1 inhibitor 22b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.429999828338623 pIC50
Reference (Journal): Identification of 5-(2,3-Dihydro-1 H-indol-5-yl)-7 H-pyrrolo[2,3- d]pyrimidin-4-amine Derivatives as a New Class of Receptor-Interacting Protein Kinase 1 (RIPK1) Inhibitors, Which Showed Potent Activity in a Tumor Metastasis Model.
Published in: J Med Chem
Target family: Kinases (<i>Plasmodium</i> spp.) (type: other_protein)
Target: Plasmodium falciparum phosphatidylinositol 4-kinase beta

Ligand: UCT943 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 pIC50
Reference (Journal): UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.
Published in: Antimicrob Agents Chemother

Ligand: compound 55 [PMID: 29889526] (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.
Published in: J Med Chem

Ligand: compound 55 [PMID: 29889526] (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.989999771118164 pIC50
Reference (Journal): Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.
Published in: J Med Chem

Ligand: CHMFL-PI4K-127 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Published in: Eur J Med Chem

Ligand: CHMFL-PI4K-127 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.050000190734863 pIC50
Reference (Journal): Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Published in: Eur J Med Chem

Ligand: CHMFL-PI4K-127 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pEC50
Reference (Journal): Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Published in: Eur J Med Chem
Target family: Kinases (<i>Plasmodium</i> spp.) (type: other_protein)
Target: Plasmodium falciparum cyclin-dependent-like kinase CLK3

Ligand: TCMDC-135051 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.489999771118164 pEC50
Reference (Journal): Validation of the protein kinase <i>Pf</i>CLK3 as a multistage cross-species malarial drug target.
Published in: Science

Ligand: TCMDC-135051 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): Validation of the protein kinase <i>Pf</i>CLK3 as a multistage cross-species malarial drug target.
Published in: Science

Ligand: TCMDC-135051 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.949999809265137 pEC50
Reference (Journal): Validation of the protein kinase <i>Pf</i>CLK3 as a multistage cross-species malarial drug target.
Published in: Science
Target family: Kinases (<i>Plasmodium</i> spp.) (type: other_protein)
Target: Plasmodium falciparum cGMP-dependent protein kinase

Ligand: MMV030084 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Published in: Cell Chem Biol

Ligand: MMV030084 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Published in: Cell Chem Biol

Ligand: MMV030084 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.960000038146973 pIC50
Reference (Journal): Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Published in: Cell Chem Biol

Ligand: MMV030084 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Published in: Cell Chem Biol

Ligand: MMV030084 (Synthetic organic)
Interaction type: None
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Published in: Cell Chem Biol

Ligand: ML10 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity: 8.680000305175781 pEC50
Reference (Journal): A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
Published in: Nat Commun

Ligand: ML10 (Synthetic organic)
Interaction type: None
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Journal): A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
Published in: Nat Commun
Target family: Kinesins (type: other_protein)
Target: kinesin-5

Ligand: AZD4877 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.
Published in: J Med Chem