dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: PIM family (type: enzyme)
Target: Pim-1 proto-oncogene, serine/threonine kinase

Ligand: SGI-1776 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Published in: J Med Chem

Ligand: silmitasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.670000076293945 pIC50
Reference (Journal): Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer.
Published in: Biochemistry

Ligand: uzansertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.619999885559082 pIC50
Reference (Journal): Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.
Published in: PLoS ONE

Ligand: voruciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.139999866485596 pIC50
Reference (Journal): Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells.
Published in: PLoS ONE
Target family: Polo-like kinase (PLK) family (type: enzyme)
Target: polo like kinase 4

Ligand: XMD8-92 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.21999979019165 pKd
Reference (Journal): Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
Published in: Cancer Cell
Target family: Polo-like kinase (PLK) family (type: enzyme)
Target: polo like kinase 3

Ligand: onvansertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Published in: Bioorg Med Chem Lett
Target family: Polo-like kinase (PLK) family (type: enzyme)
Target: polo like kinase 4

Ligand: axitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 7.340000152587891 pIC50
Reference (Journal): The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
Published in: J Med Chem

Ligand: CZS-241 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.59000015258789 pIC50
Reference (Journal): Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.
Published in: J Med Chem

Ligand: ocifisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.550000190734863 pIC50
Reference (Journal): Functional characterization of CFI-400945, a Polo-like kinase 4 inhibitor, as a potential anticancer agent.
Published in: Cancer Cell

Ligand: RG-1530 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pKd
Reference (Journal): Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.
Published in: Cell Cycle
Target family: Polo-like kinase (PLK) family (type: enzyme)
Target: polo like kinase 2

Ligand: BI-2536 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Journal): BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Published in: Curr Biol

Ligand: onvansertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: rucaparib metabolite M324 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.230000019073486 pIC50
Reference (Journal): Identification of differential biological activity and synergy between the PARP inhibitor rucaparib and its major metabolite.
Published in: Cell Chem Biol
Target family: Polo-like kinase (PLK) family (type: enzyme)
Target: polo like kinase 3

Ligand: BI-2536 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Published in: Curr Biol
Target family: Poly ADP-ribosylating PARPs (type: enzyme)
Target: tankyrase 2

Ligand: compound 5 [Tomassi et al., 2020] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): From PARP1 to TNKS2 Inhibition: A Structure-Based Approach
Published in: ACS Med Chem Lett
Target family: Poly ADP-ribosylating PARPs (type: enzyme)
Target: tankyrase

Ligand: AZ1366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Published in: ACS Med Chem Lett

Ligand: AZ6102 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Published in: ACS Med Chem Lett

Ligand: basroparib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract.
Published in: Eur J Cancer

Ligand: compound 21 [PMID: 34141085] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors.
Published in: ACS Med Chem Lett

Ligand: compound 5 [Tomassi et al., 2020] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 pIC50
Reference (Journal): From PARP1 to TNKS2 Inhibition: A Structure-Based Approach
Published in: ACS Med Chem Lett

Ligand: MC2050 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pIC50
Reference (Journal): From PARP1 to TNKS2 Inhibition: A Structure-Based Approach
Published in: ACS Med Chem Lett

Ligand: NVP‐TNKS656 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.809999942779541 pIC50
Reference (Patent): Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors

Ligand: RK-287107 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.840000152587891 pIC50
Reference (Journal): RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model.
Published in: Cancer Sci
Target family: Poly ADP-ribosylating PARPs (type: enzyme)
Target: tankyrase 2

Ligand: AZ1366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Published in: ACS Med Chem Lett

Ligand: basroparib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pIC50
Reference (Journal): Tankyrase-selective inhibitor STP1002 shows preclinical antitumour efficacy without on-target toxicity in the gastrointestinal tract.
Published in: Eur J Cancer

Ligand: compound 21 [PMID: 34141085] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors.
Published in: ACS Med Chem Lett

Ligand: MC2050 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.710000038146973 pIC50
Reference (Journal): From PARP1 to TNKS2 Inhibition: A Structure-Based Approach
Published in: ACS Med Chem Lett

Ligand: NVP‐TNKS656 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Patent): Novel 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors

Ligand: NVP‐TNKS656 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Published in: J Med Chem

Ligand: OM-1700 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.
Published in: J Med Chem

Ligand: RK-287107 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.96999979019165 pIC50
Reference (Journal): RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model.
Published in: Cancer Sci
Target family: Prokineticin receptors (type: gpcr)
Target: PKR<sub>2</sub>

Ligand: triazine compound PC10 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.92 pIC50
Reference (Journal): Prokineticin receptor 1 antagonist PC-10 as a biomarker for imaging inflammatory pain.
Published in: J Nucl Med

Ligand: triazine compound PC1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.79 pKi
Reference (Journal): Triazine compounds as antagonists at Bv8-prokineticin receptors.
Published in: J Med Chem

Ligand: [125I]BH-MIT1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.170000076293945 pIC50
Reference (Journal): Isolation and identification of EG-VEGF/prokineticins as cognate ligands for two orphan G-protein-coupled receptors.
Published in: Biochem Biophys Res Commun

Ligand: prokineticin-2β (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Identification and pharmacological characterization of prokineticin 2 beta as a selective ligand for prokineticin receptor 1.
Published in: Mol Pharmacol

Ligand: prokineticin-2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification and pharmacological characterization of prokineticin 2 beta as a selective ligand for prokineticin receptor 1.
Published in: Mol Pharmacol

Ligand: prokineticin-2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Isolation and identification of EG-VEGF/prokineticins as cognate ligands for two orphan G-protein-coupled receptors.
Published in: Biochem Biophys Res Commun

Ligand: prokineticin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Isolation and identification of EG-VEGF/prokineticins as cognate ligands for two orphan G-protein-coupled receptors.
Published in: Biochem Biophys Res Commun

Ligand: prokineticin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification and pharmacological characterization of prokineticin 2 beta as a selective ligand for prokineticin receptor 1.
Published in: Mol Pharmacol

Ligand: PKR-A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Prokineticin 2 is an endangering mediator of cerebral ischemic injury.
Published in: Proc Natl Acad Sci USA

Ligand: MIT1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): Isolation and identification of EG-VEGF/prokineticins as cognate ligands for two orphan G-protein-coupled receptors.
Published in: Biochem Biophys Res Commun
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Prolactin receptor

Ligand: prolactin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pKd
Reference (Journal): Prolactin receptors: characteristics of the particulate fraction binding activity.
Published in: J Endocrinol
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Thrombopoietin receptor

Ligand: avatrombopag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity:  -
Reference (Journal): AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist.
Published in: Eur J Haematol

Ligand: eltrombopag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
Primary target: yes
Median affinity: 7.420000076293945 pEC50
Reference (Journal): Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.
Published in: Bioorg Med Chem Lett

Ligand: hetrombopag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: China (2021)
Primary target: no
Median affinity:  -

Ligand: lusutrombopag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: Japan (2015), FDA (2018), EMA (2019)
Primary target: yes
Median affinity:  -
Reference (Journal): Development of a new knock-in mouse model and evaluation of pharmacological activities of lusutrombopag, a novel, nonpeptidyl small-molecule agonist of the human thrombopoietin receptor c-Mpl.
Published in: Exp Hematol

Ligand: romiplostim (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2009)
Primary target: yes
Median affinity:  -

Ligand: thrombopoietin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Eythropoietin receptor

Ligand: erythropoietin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1989 available)
Primary target: no
Median affinity: 11.149999618530273 pIC50
Reference (Journal): Preclinical evaluation of Hematide, a novel erythropoiesis stimulating agent, for the treatment of anemia.
Published in: Exp Hematol

Ligand: peginesatide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2012)
Primary target: yes
Median affinity: 10.430000305175781 pIC50
Reference (Journal): Preclinical evaluation of Hematide, a novel erythropoiesis stimulating agent, for the treatment of anemia.
Published in: Exp Hematol
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Granulocyte colony-stimulating factor receptor

Ligand: anumigilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.3100004196167 pKd
Reference (Patent): Antibodies against g-csfr and uses thereof

Ligand: anumigilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 8.850000381469727 pKd
Reference (Patent): Antibodies against g-csfr and uses thereof

Ligand: G-CSF (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Median affinity:  -

Ligand: pegfilgrastim (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2002)
Primary target: yes
Median affinity:  -
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Growth hormone receptor

Ligand: growth hormone 1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1976), EMA (2001)
Primary target: yes
Median affinity: 9.039999961853027 pKd
Reference (Journal): In Vitro and in Vivo Characterization of MOD-4023, a Long-Acting Carboxy-Terminal Peptide (CTP)-Modified Human Growth Hormone.
Published in: Mol Pharm

Ligand: growth hormone 2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: pegvisomant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003), EMA (2008)
Primary target: yes
Median affinity:  -
Reference (Journal): Treatment of acromegaly with the growth hormone-receptor antagonist pegvisomant.
Published in: N Engl J Med

Ligand: somatrogon (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2022), FDA (2023)
Primary target: no
Median affinity: 8.199999809265137 pKd
Reference (Journal): In Vitro and in Vivo Characterization of MOD-4023, a Long-Acting Carboxy-Terminal Peptide (CTP)-Modified Human Growth Hormone.
Published in: Mol Pharm

Ligand: somatrogon (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2022), FDA (2023)
Primary target: no
Median affinity: 8.289999961853027 pKd
Reference (Journal): In Vitro and in Vivo Characterization of MOD-4023, a Long-Acting Carboxy-Terminal Peptide (CTP)-Modified Human Growth Hormone.
Published in: Mol Pharm

Ligand: somatrogon (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2022), FDA (2023)
Primary target: no
Median affinity: 7.940000057220459 pKd
Reference (Journal): In Vitro and in Vivo Characterization of MOD-4023, a Long-Acting Carboxy-Terminal Peptide (CTP)-Modified Human Growth Hormone.
Published in: Mol Pharm
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Prolactin receptor

Ligand: choriomammotropin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: chorionic somatomammotropin hormone-like 1 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Target family: Prolactin receptor family (type: catalytic_receptor)
Target: Eythropoietin receptor

Ligand: cibinetide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Patent): Tissue protective peptides and peptide analogs for preventing and treating diseases and disorders associated with tissue damage
Target family: Prolyl hydroxylases (type: enzyme)
Target: egl-9 family hypoxia inducible factor 1

Ligand: vadadustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020), EMA (2023), FDA (2024)
Primary target: no
Median affinity: 7.539999961853027 pIC50
Reference (Journal): Inhibition of a viral prolyl hydroxylase.
Published in: Bioorg Med Chem
Target family: Prolyl hydroxylases (type: enzyme)
Target: egl-9 family hypoxia inducible factor 2

Ligand: compound 6ee [PMID: 22364528] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Published in: J Med Chem

Ligand: desidustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Novel quinolone derivatives

Ligand: molidustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Published in: J Med Chem

Ligand: roxadustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2021)
Primary target: no
Median affinity:  -
Reference (Journal): Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Published in: J Med Chem

Ligand: vadadustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020), EMA (2023), FDA (2024)
Primary target: no
Median affinity:  -
Reference (Journal): Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases.
Published in: J Med Chem
Target family: Prolyl hydroxylases (type: enzyme)
Target: egl-9 family hypoxia inducible factor 3

Ligand: compound 6ee [PMID: 22364528] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Journal): 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Published in: J Med Chem

Ligand: molidustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.309999942779541 pIC50
Reference (Patent): Substituted dihydropyrazolones for treating cardiovascular and hematological diseases.