dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 4C

Ligand: 6-Hydroxy-5,7-dimethoxyflavone (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.760000228881836 pIC50
Reference (Journal): 6-Hydroxy-5,7-dimethoxy-flavone suppresses the neutrophil respiratory burst via selective PDE4 inhibition to ameliorate acute lung injury.
Published in: Free Radic Biol Med

Ligand: apremilast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014), EMA (2015)
Primary target: yes
Median affinity: 6.929999828338623 pIC50
Reference (Journal): Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity.
Published in: Cell Signal

Ligand: CDP840 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pKi
Reference (Journal): CDP840: a novel inhibitor of PDE-4.
Published in: Cell Biochem Biophys

Ligand: ibudilast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: yes
Median affinity: 6.619999885559082 pIC50
Reference (Journal): Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
Published in: J Med Chem

Ligand: MK-0359 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.039999961853027 pIC50
Reference (Journal): L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition.
Published in: Biochem Pharmacol

Ligand: Ro20-1724 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
Published in: Biochem Biophys Res Commun

Ligand: rolipram (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D.
Published in: Biochem Biophys Res Commun

Ligand: RS-25344 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Comparison of recombinant human PDE4 isoforms: interaction with substrate and inhibitors.
Published in: Cell Signal
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 5A

Ligand: compound 3m [PMID: 32603117] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.429999828338623 pIC50
Reference (Journal): Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.
Published in: J Med Chem
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 10A

Ligand: compound 19 [PMID: 22142545] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pKi
Reference (Journal): Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 22142545] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pKi
Reference (Journal): Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
Published in: Bioorg Med Chem Lett
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 8A

Ligand: dipyridamole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 5.1 pIC50
Reference (Journal): Isolation and characterization of PDE8A, a novel human cAMP-specific phosphodiesterase.
Published in: Biochem Biophys Res Commun

Ligand: PF-04957325 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.369999885559082 pIC50
Reference (Journal): Advances in targeting cyclic nucleotide phosphodiesterases.
Published in: Nat Rev Drug Discov
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 8B

Ligand: dipyridamole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Median affinity: 4.3 pIC50
Reference (Journal): Molecular cloning and characterization of human PDE8B, a novel thyroid-specific isozyme of 3',5'-cyclic nucleotide phosphodiesterase.
Published in: Biochem Biophys Res Commun
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 9A

Ligand: SCH51866 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): Isolation and characterization of PDE9A, a novel human cGMP-specific phosphodiesterase.
Published in: J Biol Chem

Ligand: zaprinast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.5 pIC50
Reference (Journal): Isolation and characterization of PDE9A, a novel human cGMP-specific phosphodiesterase.
Published in: J Biol Chem
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 6A

Ligand: compound 53 [PMID: 19631533] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 pIC50
Reference (Journal): Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Published in: Bioorg Med Chem Lett
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 6C

Ligand: PDE4 inhibitor 16 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.480000019073486 pIC50
Reference (Journal): Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Published in: J Med Chem

Ligand: sildenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1998)
Primary target: no
Median affinity: 7.409999847412109 pIC50
Reference (Journal): Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Published in: J Med Chem
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 7A

Ligand: BRL50481 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): New classes of PDE7 inhibitors identified by a fission yeast-based HTS.
Published in: J Biomol Screen

Ligand: BRL50481 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes.
Published in: Mol Pharmacol

Ligand: crisaborole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2016), EMA (2020)
Primary target: no
Median affinity: 6.139999866485596 pIC50
Reference (Journal): Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
Published in: Bioorg Med Chem Lett
Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 7B

Ligand: BRL50481 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 4.9 pIC50
Reference (Journal): New classes of PDE7 inhibitors identified by a fission yeast-based HTS.
Published in: J Biomol Screen

Ligand: dipyridamole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pIC50
Reference (Journal): Identification of human PDE7B, a cAMP-specific phosphodiesterase.
Published in: Biochem Biophys Res Commun

Ligand: dipyridamole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1961)
Median affinity:  pIC50
Reference (Journal): Cloning and characterization of the human and mouse PDE7B, a novel cAMP-specific cyclic nucleotide phosphodiesterase.
Published in: Biochem Biophys Res Commun

Ligand: SCH51866 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 5.8 pIC50
Reference (Journal): Identification of human PDE7B, a cAMP-specific phosphodiesterase.
Published in: Biochem Biophys Res Commun
Target family: Phosphodiesterases (other) (type: enzyme)
Target: phosphodiesterase 12

Ligand: compound 1 [PMID: 26055709] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors.
Published in: J Biol Chem

Ligand: compound 3 [PMID: 26055709] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.760000228881836 pKi
Reference (Journal): The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors.
Published in: J Biol Chem

Ligand: compound 3 [PMID: 26055709] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pIC50
Reference (Journal): The Role of Phosphodiesterase 12 (PDE12) as a Negative Regulator of the Innate Immune Response and the Discovery of Antiviral Inhibitors.
Published in: J Biol Chem
Target family: Phosphoinositide-specific phospholipase C (type: enzyme)
Target: PLC&gamma;2

Ligand: CCT129957 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): The identification of novel PLC-gamma inhibitors using virtual high throughput screening.
Published in: Bioorg Med Chem
Target family: Phosphoinositide-specific phospholipase C (type: enzyme)
Target: PLC&gamma;1

Ligand: compound 5 [PMID: 10869194] (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.019999980926514 pIC50
Reference (Journal): Inhibition of phospholipase cgamma1 and cancer cell proliferation by triterpene esters from Uncaria rhynchophylla.
Published in: J Nat Prod
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-1B

Ligand: compound 28xvii [PMID: 8809154] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-2F

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-2E

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-2D

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-2A

Ligand: varespladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
Published in: J Med Chem

Ligand: varespladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
Published in: J Med Chem

Ligand: varespladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Pharmacology of LY315920/S-5920, [[3-(aminooxoacetyl)-2-ethyl-1- (phenylmethyl)-1H-indol-4-yl]oxy] acetate, a potent and selective secretory phospholipase A2 inhibitor: A new class of anti-inflammatory drugs, SPI.
Published in: J Pharmacol Exp Ther

Ligand: KH064 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A2 (IIa) with antiinflammatory activity.
Published in: Chembiochem

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-1B

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: sPLA<sub>2</sub>-10

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: PLA<sub>2</sub>-G7

Ligand: rilapladib (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 9.640000343322754 pIC50
Reference (Journal): Lipoprotein-associated phospholipase A(2) and atherosclerosis.
Published in: Curr Opin Lipidol

Ligand: (S)-23 [PMID: 27933945] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Published in: J Med Chem

Ligand: (S)-23 [PMID: 27933945] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Published in: J Med Chem

Ligand: darapladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.3100004196167 pIC50
Reference (Journal): Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Published in: J Med Chem

Ligand: darapladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2).
Published in: J Med Chem

Ligand: darapladib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.960000038146973 pIC50
Reference (Journal): The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.
Published in: Bioorg Med Chem Lett

Ligand: compound 37 [PMID: 29193967] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2.
Published in: J Med Chem

Ligand: ABX-1431 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: PLA<sub>2</sub>-G5

Ligand: compound 12e [PMID: 18605714] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pIC50
Reference (Journal): Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Published in: J Med Chem
Target family: Phospholipase A<sub>2</sub> (type: enzyme)
Target: cPLA<sub>2</sub>-4A

Ligand: compound 57 [PMID: 16610804] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.369999885559082 pIC50
Reference (Journal): Design and synthesis of 1-indol-1-yl-propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha.
Published in: J Med Chem
Target family: Phosphorylase kinase (PHK) family (type: enzyme)
Target: phosphorylase kinase catalytic subunit gamma 2

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 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: compound 2c [PMID: 24900538] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 pIC50
Reference (Journal): Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
Published in: ACS Med Chem Lett
Target family: Phosphorylase kinase (PHK) family (type: enzyme)
Target: phosphorylase kinase catalytic subunit gamma 1

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: Piezo channels (type: other_ic)
Target: Piezo1

Ligand: Jedi1 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A lever-like transduction pathway for long-distance chemical- and mechano-gating of the mechanosensitive Piezo1 channel.
Published in: Nat Commun

Ligand: Dooku1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pIC50
Reference (Journal): Yoda1 analogue (Dooku1) which antagonizes Yoda1-evoked activation of Piezo1 and aortic relaxation.
Published in: Br J Pharmacol

Ligand: Dooku1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pIC50
Reference (Journal): Yoda1 analogue (Dooku1) which antagonizes Yoda1-evoked activation of Piezo1 and aortic relaxation.
Published in: Br J Pharmacol

Ligand: Yoda1 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.769999980926514 pEC50
Reference (Journal): Chemical activation of the mechanotransduction channel Piezo1.
Published in: Elife

Ligand: Yoda1 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: yes
Median affinity: 4.579999923706055 pEC50
Reference (Journal): Chemical activation of the mechanotransduction channel Piezo1.
Published in: Elife

Ligand: Jedi2 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: yes
Median affinity: 3.799999952316284 pEC50
Reference (Journal): A lever-like transduction pathway for long-distance chemical- and mechano-gating of the mechanosensitive Piezo1 channel.
Published in: Nat Commun
Target family: PIM family (type: enzyme)
Target: Pim-2 proto-oncogene, serine/threonine kinase

Ligand: AZD1208 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.800000190734863 pKi
Reference (Journal): Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Published in: ACS Med Chem Lett

Ligand: compound 14k [PMID: 21982499] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pIC50
Reference (Journal): 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Published in: Bioorg Med Chem Lett
Target family: PIM family (type: enzyme)
Target: Pim-1 proto-oncogene, serine/threonine kinase

Ligand: compound 14k [PMID: 21982499] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Published in: Bioorg Med Chem Lett