dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: MSN subfamily (type: enzyme)
Target: mitogen-activated protein kinase kinase kinase kinase 4

Ligand: compound 12k [PMID: 31676236] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents.
Published in: Cell Chem Biol

Ligand: compound 21 [PMID: 23312943] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Published in: Bioorg Med Chem Lett

Ligand: compound 26 [PMID: 24673130] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.769999980926514 pIC50
Reference (Journal): Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.
Published in: J Med Chem

Ligand: PF06260933 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pIC50
Reference (Journal): 2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.
Published in: J Med Chem
Target family: MSN subfamily (type: enzyme)
Target: TRAF2 and NCK interacting kinase

Ligand: compound 21k [PMID: 34985886] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pIC50
Reference (Journal): Discovery of 3,4-Dihydrobenzo[<i>f</i>][1,4]oxazepin-5(2<i>H</i>)-one Derivatives as a New Class of Selective TNIK Inhibitors and Evaluation of Their Anti-Colorectal Cancer Effects.
Published in: J Med Chem

Ligand: compound 25c [PMID: 36649216] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Discovery of Novel Indazole Chemotypes as Isoform-Selective JNK3 Inhibitors for the Treatment of Parkinson's Disease.
Published in: J Med Chem

Ligand: compound 5 [PMID: 23232060] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: INS018_055 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models.
Published in: Nat Biotechnol

Ligand: INS018_055 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.359999656677246 pKd
Reference (Journal): A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models.
Published in: Nat Biotechnol

Ligand: PF06260933 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.
Published in: ACS Med Chem Lett

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pIC50
Reference (Journal): Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors.
Published in: Bioorg Med Chem Lett
Target family: MST subfamily (type: enzyme)
Target: serine/threonine kinase 3

Ligand: CEP-11981 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pIC50
Reference (Journal): Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Published in: J Med Chem
Target family: MST subfamily (type: enzyme)
Target: serine/threonine kinase 4

Ligand: cerdulatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancer.
Published in: J Pharmacol Exp Ther

Ligand: XMU-MP-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.309999942779541 pIC50
Reference (Journal): Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Published in: J Med Chem

Ligand: SBP-3264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pIC50
Reference (Journal): Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Published in: J Med Chem

Ligand: IHMT-MST1-58 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes.
Published in: J Med Chem

Ligand: compound 38 [PMID: 20817473] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pIC50
Reference (Journal): Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.
Published in: Bioorg Med Chem

Ligand: bosutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Published in: Leukemia
Target family: MST subfamily (type: enzyme)
Target: serine/threonine kinase 3

Ligand: XMU-MP-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.789999961853027 pIC50
Reference (Journal): Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Published in: J Med Chem

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.390000343322754 pIC50
Reference (Journal): Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
Published in: J Med Chem

Ligand: SBP-3264 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pIC50
Reference (Journal): Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.
Published in: J Med Chem
Target family: Myosin Light Chain Kinase (MLCK) family (type: enzyme)
Target: myosin light chain kinase

Ligand: RKI-1447 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.809999942779541 pIC50
Reference (Journal): Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
Published in: Medchemcomm

Ligand: calmodulin (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Human platelet myosin light chain kinase requires the calcium-binding protein calmodulin for activity.
Published in: Proc Natl Acad Sci USA
Target family: Myosin Light Chain Kinase (MLCK) family (type: enzyme)
Target: myosin light chain kinase family member 4

Ligand: compound 17 [PMID: 36111834] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.579999923706055 pIC50
Reference (Journal): Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of &#x3b2;-Coronaviruses.
Published in: J Med Chem
Target family: Myosin Light Chain Kinase (MLCK) family (type: enzyme)
Target: myosin light chain kinase 2

Ligand: GSK2606414 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Published in: J Med Chem

Ligand: calmodulin (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Median affinity:  -
Reference (Journal): Human platelet myosin light chain kinase requires the calcium-binding protein calmodulin for activity.
Published in: Proc Natl Acad Sci USA
Target family: Myosin Light Chain Kinase (MLCK) family (type: enzyme)
Target: myosin light chain kinase

Ligand: MLCK inhibitor peptide 18 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge.
Published in: J Med Chem
Target family: N6-methyladenosine readers (type: other_protein)
Target: YTH N6-methyladenosine RNA binding protein C1

Ligand: YTHDC1 inhibitor 40 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.309999942779541 pKd
Reference (Journal): Structure-Based Design of a Potent and Selective YTHDC1 Ligand.
Published in: J Med Chem
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 5

Ligand: setanaxib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pKi
Reference (Journal): Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent.
Published in: Hepatology
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 4

Ligand: compound 87 [PMID: 20942471] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.329999923706055 pKi
Reference (Journal): First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.
Published in: J Med Chem

Ligand: compound 7c [PMID: 22041175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.139999866485596 pKi
Reference (Journal): Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.
Published in: Bioorg Med Chem
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 1

Ligand: setanaxib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.849999904632568 pKi
Reference (Journal): Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent.
Published in: Hepatology

Ligand: NSC 780521 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.989999771118164 pIC50
Reference (Journal): Characterization of potent and selective iodonium-class inhibitors of NADPH oxidases.
Published in: Biochem Pharmacol

Ligand: GKT136901 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.800000190734863 pKi
Reference (Journal): First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.
Published in: J Med Chem

Ligand: compound 7c [PMID: 22041175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.
Published in: Bioorg Med Chem
Target family: NADPH oxidases (type: enzyme)
Target: dual oxidase 2

Ligand: NSC 780521 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.110000133514404 pIC50
Reference (Journal): Characterization of potent and selective iodonium-class inhibitors of NADPH oxidases.
Published in: Biochem Pharmacol
Target family: NADPH oxidases (type: enzyme)
Target: cytochrome b-245 beta chain

Ligand: setanaxib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.760000228881836 pKi
Reference (Journal): Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent.
Published in: Hepatology

Ligand: NSC 780521 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.980000019073486 pIC50
Reference (Journal): Characterization of potent and selective iodonium-class inhibitors of NADPH oxidases.
Published in: Biochem Pharmacol

Ligand: GKT136901 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pKi
Reference (Journal): First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.
Published in: J Med Chem

Ligand: compound 7c [PMID: 22041175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.869999885559082 pKi
Reference (Journal): Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.
Published in: Bioorg Med Chem
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 4

Ligand: setanaxib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.960000038146973 pKi
Reference (Journal): Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent.
Published in: Hepatology
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 5

Ligand: compound 7c [PMID: 22041175] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.380000114440918 pKi
Reference (Journal): Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.
Published in: Bioorg Med Chem

Ligand: NSC 780521 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.639999866485596 pIC50
Reference (Journal): Characterization of potent and selective iodonium-class inhibitors of NADPH oxidases.
Published in: Biochem Pharmacol
Target family: NADPH oxidases (type: enzyme)
Target: NADPH oxidase 4

Ligand: GKT136901 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.78000020980835 pKi
Reference (Journal): First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.
Published in: J Med Chem
Target family: NAK family (type: enzyme)
Target: AP2 associated kinase 1

Ligand: compound 6 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem

Ligand: compound 13 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem

Ligand: BMS-911172 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Discovery, Structure-Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain.
Published in: J Med Chem

Ligand: baricitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2017), FDA (2018)
Primary target: no
Median affinity: 7.769999980926514 pKd
Reference (Journal): COVID-19: combining antiviral and anti-inflammatory treatments.
Published in: Lancet Infect Dis
Target family: NAK family (type: enzyme)
Target: serine/threonine kinase 16

Ligand: STK16-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.53000020980835 pIC50
Reference (Journal): Discovery of a Highly Selective STK16 Kinase Inhibitor.
Published in: ACS Chem Biol

Ligand: compound 6 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.059999942779541 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem

Ligand: compound 27 [PMID: 21123062] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 13 [PMID: 34333981] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.090000152587891 pIC50
Reference (Journal): Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Published in: J Med Chem
Target family: NAK family (type: enzyme)
Target: AP2 associated kinase 1

Ligand: pilavapadin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Published in: J Med Chem

Ligand: compound 21b [PMID: 31136173] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.
Published in: J Med Chem
Target family: Na<sup>+</sup>/K<sup>+</sup>-ATPases (type: transporter)
Target: sodium/potassium-transporting ATPase subunit &alpha;-1

Ligand: digoxin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (no history prior to 1975)
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Structure-based design and synthesis of novel potent Na+,K+ -ATPase inhibitors derived from a 5alpha,14alpha-androstane scaffold as positive inotropic compounds.
Published in: J Med Chem

Ligand: digoxin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (no history prior to 1975)
Primary target: yes
Median affinity:  -

Ligand: deslanoside (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity:  -

Ligand: digitoxin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Synthesis of 20-hydroxy-, 20-amino-, and 20-nitro-14-hydroxy-21-nor-5 beta,14 beta-pregnane C-3 glycosides and related derivatives: structure-activity relationships of pregnanes that bind to the digitalis receptor.
Published in: J Med Chem

Ligand: digitoxin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity:  -

Ligand: acetyldigitoxin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009)
Primary target: yes
Median affinity:  -
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 2

Ligand: lestaurtinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 1

Ligand: sunitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: no
Median affinity: 6.199999809265137 pKd
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 2

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.420000076293945 pIC50
Reference (Journal): ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
Published in: Eur J Med Chem

Ligand: sunitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: no
Median affinity: 6.340000152587891 pKd
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood

Ligand: TRULI (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Small-molecule inhibition of Lats kinases may promote Yap-dependent proliferation in postmitotic mammalian tissues.
Published in: Nat Commun