dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Heat shock proteins (type: other_protein)
Target: heat shock protein 90 alpha family class A member 1

Ligand: alvespimycin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.
Published in: Bioorg Med Chem Lett

Ligand: BIIB021 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
Published in: Bioorg Med Chem Lett

Ligand: ganetespib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): K4DD drug target binding kinetics data

Ligand: ganetespib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.
Published in: J Med Chem

Ligand: retaspimycin hydrochloride (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pEC50
Reference (Journal): Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
Published in: J Med Chem

Ligand: SNX0723 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
Published in: Bioorg Med Chem Lett
Target family: Heat shock proteins (type: other_protein)
Target: heat shock protein 90 alpha family class B member 1

Ligand: geldanamycin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.
Published in: Bioorg Med Chem

Ligand: luminespib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Target family: Heat shock proteins (type: other_protein)
Target: heat shock protein 90 beta family member 1

Ligand: semapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Experimental Anti-Inflammatory Drug Semapimod Inhibits TLR Signaling by Targeting the TLR Chaperone gp96.
Published in: J Immunol

Ligand: compound 18c [PMID: 25901531] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.659999847412109 pIC50
Reference (Journal): Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.
Published in: J Med Chem

Ligand: Grp94 inhibitor 54 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
Published in: J Med Chem
Target family: Hexokinases (type: enzyme)
Target: Glucokinase

Ligand: AZD1656 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: yes
Median affinity: 7.239999771118164 pEC50
Reference (Webpage): AZD1656.

Ligand: dorzagliatin (Synthetic organic)
Interaction type: Allosteric modulator
Action: Activation
Ligand approved: yes
Approval source: China (2022)
Primary target: no
Median affinity:  -
Reference (Journal): Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus.
Published in: J Diabetes Res

Ligand: BMS-820132 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1<i>H</i>-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Published in: J Med Chem
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 1

Ligand: remogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi
Reference (Journal): Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models.
Published in: J Pharmacol Exp Ther

Ligand: mizagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.570000171661377 pKi
Reference (Journal): Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation.
Published in: Eur J Pharmacol

Ligand: licogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Patent): Glycoside derivatives and uses thereof

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 5.929999828338623 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 5.730000019073486 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 5.860000133514404 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ertugliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 5.710000038146973 pIC50
Reference (Journal): Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Published in: J Med Chem
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 2

Ligand: canagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2013)
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.
Published in: PLoS ONE

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 8.25 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 1

Ligand: enavogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.260000228881836 pIC50
Reference (Journal): Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin.
Published in: Pharmaceutics

Ligand: empagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 5.099999904632568 pIC50
Reference (Journal): Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors.
Published in: Diabetes Obes Metab

Ligand: dapagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2012), FDA (2014)
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Discovery of non-glucoside SGLT2 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: canagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2013)
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.
Published in: PLoS ONE

Ligand: bexagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: no
Median affinity: 5.25 pIC50
Reference (Journal): C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Published in: Bioorg Med Chem Lett
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 2

Ligand: empagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: yes
Median affinity: 8.5 pIC50
Reference (Journal): Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors.
Published in: Diabetes Obes Metab

Ligand: dapagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2012), FDA (2014)
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors.
Published in: Bioorg Med Chem

Ligand: ipragliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: yes
Median affinity: 8.130000114440918 pIC50
Reference (Journal): Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: bexagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: yes
Median affinity: 8.640000343322754 pIC50
Reference (Journal): C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Published in: Bioorg Med Chem Lett
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 1

Ligand: tofogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: no
Median affinity: 5.070000171661377 pIC50
Reference (Journal): Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: sotagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2019), FDA (2023)
Primary target: yes
Median affinity: 7.440000057220459 pIC50
Reference (Journal): LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial.
Published in: Clin Pharmacol Ther

Ligand: sergliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level.
Published in: J Pharmacol Exp Ther
Target family: Hexose transporter family (type: transporter)
Target: Sodium/glucose cotransporter 2

Ligand: ertugliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: yes
Median affinity: 9.0600004196167 pIC50
Reference (Journal): Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Published in: J Med Chem

Ligand: enavogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin.
Published in: Pharmaceutics

Ligand: tofogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014)
Primary target: yes
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Discovery of tofogliflozin, a novel C-arylglucoside with an O-spiroketal ring system, as a highly selective sodium glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: sotagliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2019), FDA (2023)
Primary target: yes
Median affinity: 8.739999771118164 pIC50
Reference (Journal): LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial.
Published in: Clin Pharmacol Ther

Ligand: sergliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.800000190734863 pKi
Reference (Journal): Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level.
Published in: J Pharmacol Exp Ther

Ligand: remogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.900000095367432 pKi
Reference (Journal): Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models.
Published in: J Pharmacol Exp Ther

Ligand: licogliflozin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Patent): Glycoside derivatives and uses thereof
Target family: HH498 subfamily (type: enzyme)
Target: TNNI3 interacting kinase

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 6.550000190734863 pKd
Reference (Journal): A quantitative analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: GSK329 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Published in: J Med Chem

Ligand: GSK329 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pKi
Reference (Journal): Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Published in: J Med Chem

Ligand: GSK329 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.270000457763672 pKi
Reference (Journal): Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf.
Published in: J Med Chem

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 6.550000190734863 pKd
Reference (Journal): A small molecule-kinase interaction map for clinical kinase inhibitors.
Published in: Nat Biotechnol
Target family: High Mobility Group (HMG) proteins (type: other_protein)
Target: high mobility group box 1

Ligand: methotrexate (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1953), EMA (2016)
Primary target: no
Median affinity: 7.619999885559082 pKd
Reference (Journal): High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target.
Published in: J Med Chem

Ligand: 3-AESA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.829999923706055 pKd
Reference (Journal): High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target.
Published in: J Med Chem
Target family: HIPK subfamily (type: enzyme)
Target: homeodomain interacting protein kinase 1

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.579999923706055 pIC50
Reference (Journal): Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
Published in: J Med Chem
Target family: HIPK subfamily (type: enzyme)
Target: homeodomain interacting protein kinase 3

Ligand: silmitasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.349999904632568 pIC50
Reference (Journal): Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer.
Published in: J Med Chem
Target family: HIPK subfamily (type: enzyme)
Target: homeodomain interacting protein kinase 2

Ligand: compound 5b [PMID: 24900464] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
Published in: ACS Med Chem Lett

Ligand: compound 1a [PMID: 24900749] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Published in: ACS Med Chem Lett
Target family: Histamine receptors (type: gpcr)
Target: H<sub>3</sub> receptor

Ligand: ST-1006 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
Published in: Pharmacol Rev
Target family: H<sup>+</sup>/K<sup>+</sup>-ATPases (type: transporter)
Target: ATP4A

Ligand: revaprazan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: S Korea (2007)
Primary target: no
Median affinity: 6.460000038146973 pIC50
Reference (Journal): Novel pyrimidines as acid pump antagonists (APAs).
Published in: Bioorg Med Chem Lett

Ligand: tegoprazan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: S Korea (2018)
Primary target: no
Median affinity: 6.28000020980835 pIC50
Reference (Journal): Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility.
Published in: J Pharmacol Exp Ther

Ligand: vonoprazan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2014), FDA (2022)
Primary target: no
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB).
Published in: J Med Chem

Ligand: esomeprazole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2001), EMA (2013)
Primary target: yes
Median affinity:  -

Ligand: ilaprazole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: South Korea, China
Primary target: no
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo.
Published in: Arzneimittelforschung

Ligand: omeprazole (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity:  -

Ligand: revaprazan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: S Korea (2007)
Primary target: no
Median affinity: 5.639999866485596 pIC50
Reference (Journal): Structural Basis for Binding of Potassium-Competitive Acid Blockers to the Gastric Proton Pump.
Published in: J Med Chem
Target family: Human endogenous retrovirus (HERV) proteins (type: other_protein)
Target: endogenous retrovirus group W member 1, envelope

Ligand: temelimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.65999984741211 pKd
Reference (Journal): Preclinical and early clinical development of GNbAC1, a humanized IgG4 monoclonal antibody targeting endogenous retroviral MSRV-Env protein.
Published in: MAbs
Target family: HUNK subfamily (type: enzyme)
Target: hormonally up-regulated Neu-associated kinase

Ligand: HSL119 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer.
Published in: Cell Chem Biol