dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: S8: Subtilisin (type: enzyme)
Target: proprotein convertase subtilisin/kexin type 9

Ligand: alirocumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: yes
Median affinity: 9.420000076293945 pKd
Reference (Patent): High affinity human antibodies to PCSK9.

Ligand: AZD0780 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKd
Reference (Patent): PCSK9 inhibitors and methods of use thereof

Ligand: bococizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 10 pKd
Reference (Patent): Isolated antibody which specifically binds to PCSK9.

Ligand: compound 16 [PMID: 31653597] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 6.96999979019165 pKi
Reference (Journal): From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Published in: Cell Chem Biol

Ligand: evolocumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: yes
Median affinity: 9.720000267028809 pKd
Reference (Patent): Antigen binding proteins to proprotein convertase subtilisin kexin type 9 (PCSK9).

Ligand: MK-0616 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 11.300000190734863 pKi
Reference (Journal): Orally Bioavailable Macrocyclic Peptide That Inhibits Binding of PCSK9 to the Low Density Lipoprotein Receptor.
Published in: Circulation
Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: dipeptidyl peptidase 4

Ligand: linagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2011)
Primary target: yes
Median affinity: 9 pKi
Reference (Journal): 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.
Published in: J Med Chem
Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: prolyl endopeptidase like

Ligand: compound 8 [PMID: 21692504] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pIC50
Reference (Journal): A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors.
Published in: J Am Chem Soc
Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: prolyl endopeptidase

Ligand: S 17092 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
Published in: J Med Chem

Ligand: poststatin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues.
Published in: J Antibiot

Ligand: ARI-3531 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
Published in: J Med Chem
Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: fibroblast activation protein alpha

Ligand: compound 9 [PMID: 20718420] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
Published in: J Med Chem

Ligand: ARI-3099 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.440000057220459 pIC50
Reference (Journal): Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
Published in: J Med Chem
Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: acylaminoacyl-peptide hydrolase

Ligand: ARI-3099 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 pIC50
Reference (Journal): A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.
Published in: Nat Chem Biol
Target family: Scavenger receptors (type: other_protein)
Target: stabilin 1

Ligand: bexmarilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pKd
Reference (Journal): Nonclinical Characterization of Bexmarilimab, a Clever-1-Targeting Antibody for Supporting Immune Defense Against Cancers.
Published in: Mol Cancer Ther

Ligand: bexmarilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.039999961853027 pKd
Reference (Journal): Nonclinical Characterization of Bexmarilimab, a Clever-1-Targeting Antibody for Supporting Immune Defense Against Cancers.
Published in: Mol Cancer Ther
Target family: Selenoenzymes (type: enzyme)
Target: glutathione peroxidase 4

Ligand: GPX4 inhibitor C18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Discovery of Novel Potent Covalent Glutathione Peroxidase 4 Inhibitors as Highly Selective Ferroptosis Inducers for the Treatment of Triple-Negative Breast Cancer.
Published in: J Med Chem

Ligand: ML162 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 pIC50
Reference (Journal): Discovery of Novel Potent Covalent Glutathione Peroxidase 4 Inhibitors as Highly Selective Ferroptosis Inducers for the Treatment of Triple-Negative Breast Cancer.
Published in: J Med Chem
Target family: Serine palmitoyltransferase (type: enzyme)
Target: serine palmitoyltransferase long chain base subunit 1

Ligand: myriocin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.550000190734863 pKi
Reference (Journal): Serine palmitoyltransferase is the primary target of a sphingosine-like immunosuppressant, ISP-1/myriocin.
Published in: Biochem Biophys Res Commun
Target family: Serine palmitoyltransferase (type: enzyme)
Target: serine palmitoyltransferase long chain base subunit 2

Ligand: myriocin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Serine palmitoyltransferase is the primary target of a sphingosine-like immunosuppressant, ISP-1/myriocin.
Published in: Biochem Biophys Res Commun
Target family: Serine palmitoyltransferase (type: enzyme)
Target: serine palmitoyltransferase long chain base subunit 3

Ligand: myriocin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Serine palmitoyltransferase is the primary target of a sphingosine-like immunosuppressant, ISP-1/myriocin.
Published in: Biochem Biophys Res Commun
Target family: Serine palmitoyltransferase (type: enzyme)
Target: serine palmitoyltransferase small subunit B

Ligand: compound 18 [PMID: 32330443] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.769999980926514 pKi
Reference (Journal): Combined Omics Approach Identifies Gambogic Acid and Related Xanthones as Covalent Inhibitors of the Serine Palmitoyltransferase Complex.
Published in: Cell Chem Biol
Target family: Serum pentraxins (type: other_protein)
Target: amyloid P component, serum

Ligand: miridesap (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Selective optimization of side activities: another way for drug discovery.
Published in: J Med Chem

Ligand: dezamizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Antibodies to human serum amyloid P component eliminate visceral amyloid deposits.
Published in: Nature
Target family: SGK family (type: enzyme)
Target: serum/glucocorticoid regulated kinase 1

Ligand: EMD638683 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.519999980926514 pIC50
Reference (Journal): EMD638683, a novel SGK inhibitor with antihypertensive potency.
Published in: Cell Physiol Biochem

Ligand: GSK650394 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.210000038146973 pIC50
Reference (Journal): Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic.
Published in: Cancer Res

Ligand: PO-322 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.269999980926514 pIC50
Reference (Journal): PO-322 exerts potent immunosuppressive effects in vitro and in vivo by selectively inhibiting SGK1 activity.
Published in: Br J Pharmacol

Ligand: Sanofi-14h (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Published in: ACS Med Chem Lett
Target family: SGK family (type: enzyme)
Target: serum/glucocorticoid regulated kinase 2

Ligand: GSK650394 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.989999771118164 pIC50
Reference (Journal): Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic.
Published in: Cancer Res

Ligand: privosegtor (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation.
Published in: Neurotherapeutics
Target family: SGK family (type: enzyme)
Target: serum/glucocorticoid regulated kinase family member 3

Ligand: Sanofi-14h (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50

Ligand: compound 14n [PMID: 25589934] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.510000228881836 pIC50
Reference (Journal): Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Published in: ACS Med Chem Lett
Target family: SGK family (type: enzyme)
Target: serum/glucocorticoid regulated kinase 2

Ligand: compound 14n [PMID: 25589934] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Published in: ACS Med Chem Lett
Target family: SGK family (type: enzyme)
Target: serum/glucocorticoid regulated kinase 1

Ligand: Sanofi-14h (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour&#xa0;growth.
Published in: EMBO J

Ligand: compound 14n [PMID: 25589934] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Published in: ACS Med Chem Lett
Target family: SIGLECs (conserved) (type: other_protein)
Target: CD22

Ligand: moxetumomab pasudotox (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2018), EMA (2021)
Primary target: yes
Median affinity: 8.220000267028809 pKd
Reference (Journal): Antibody fusion proteins: anti-CD22 recombinant immunotoxin moxetumomab pasudotox.
Published in: Clin Cancer Res

Ligand: moxetumomab pasudotox (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2018), EMA (2021)
Primary target: yes
Median affinity: 8.220000267028809 pKd
Reference (Journal): Phase I trial of anti-CD22 recombinant immunotoxin moxetumomab pasudotox (CAT-8015 or HA22) in patients with hairy cell leukemia.
Published in: J Clin Oncol

Ligand: inotuzumab ozogamicin (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2017)
Primary target: yes
Median affinity: 9.699999809265137 pKd
Reference (Journal): Antibody-targeted chemotherapy with CMC-544: a CD22-targeted immunoconjugate of calicheamicin for the treatment of B-lymphoid malignancies.
Published in: Blood

Ligand: moxetumomab pasudotox (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2018), EMA (2021)
Primary target: yes
Median affinity: 8.220000267028809 pKd
Reference (Patent): Mutated anti-cd22 antibodies with increased affinity to cd22-expressing leukemia cells.
Target family: Sigma receptors (type: other_protein)
Target: &sigma;2

Ligand: vanoxerine (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain.
Published in: Life Sci

Ligand: [3H]-di-o-tolylguanidine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: SM 21 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors.
Published in: Life Sci

Ligand: PD-144418 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.860000133514404 pKi
Reference (Journal): The pharmacology of the novel and selective sigma ligand, PD 144418.
Published in: Neuropharmacology

Ligand: PB-28 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
Published in: J Med Chem

Ligand: CT1812 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pKi
Reference (Journal): Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer's Disease.
Published in: ACS Med Chem Lett

Ligand: 1,3-ditolylguanidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503.
Published in: Synapse
Target family: Signal regulatory proteins (type: other_protein)
Target: SIRPA (CD172a)

Ligand: thrombospondin 1 (Peptide)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: SLC10 family of sodium-bile acid co-transporters (type: transporter)
Target: Sodium/bile acid and sulphated solute cotransporter 1

Ligand: bulevirtide (Peptide)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: EMA (2020), UK HMRA (2021)
Primary target: no
Median affinity:  -

Ligand: cyclosporin A (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and UK (1983), EMA (2015)
Primary target: no
Median affinity: 5.119999885559082 pKi
Reference (Journal): Structure-activity relationship for FDA approved drugs as inhibitors of the human sodium taurocholate cotransporting polypeptide (NTCP).
Published in: Mol Pharm

Ligand: cyclosporin A (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and UK (1983), EMA (2015)
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Published in: J Pharmacol Exp Ther

Ligand: irbesartan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1997)
Primary target: no
Median affinity: 4.920000076293945 pKi
Reference (Journal): Structure-activity relationship for FDA approved drugs as inhibitors of the human sodium taurocholate cotransporting polypeptide (NTCP).
Published in: Mol Pharm

Ligand: (+)-propranolol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.260000228881836 pIC50
Reference (Journal): Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Published in: J Pharmacol Exp Ther

Ligand: (-)-propranolol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.210000038146973 pIC50
Reference (Journal): Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Published in: J Pharmacol Exp Ther

Ligand: ursodeoxycholic acid (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: UK (2003)
Primary target: no
Median affinity: 5.440000057220459 pIC50
Reference (Journal): Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity.
Published in: J Pharmacol Exp Ther
Target family: SLC10 family of sodium-bile acid co-transporters (type: transporter)
Target: Sodium/bile acid and sulphated solute cotransporter 2

Ligand: 264W94 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.32 pIC50
Reference (Journal): A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.
Published in: Bioorg Med Chem Lett

Ligand: 264W94 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.32 pIC50
Reference (Journal): Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: elobixibat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2018)
Primary target: no
Median affinity: 8.920000076293945 pIC50
Reference (Patent): Ibat inhibitors for the treatment of liver diseases

Ligand: maralixibat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: no
Median affinity: 9.550000190734863 pIC50
Reference (Journal): Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 2).
Published in: J Med Chem

Ligand: odevixibat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2021)
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Patent): IBAT inhibitors for the treatment of liver disease

Ligand: SC-435 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.82 pIC50
Reference (Journal): Inhibition of ileal bile acid transport and reduced atherosclerosis in apoE-/- mice by SC-435.
Published in: J Lipid Res

Ligand: [3H]taurocholic acid (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Reference (Journal): Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter.
Published in: Am J Physiol
Target family: SLC11 family of proton-coupled metal ion transporters (type: transporter)
Target: DMT1

Ligand: compound 6b [PMID: 22749870] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Discovery of benzylisothioureas as potent divalent metal transporter 1 (DMT1) inhibitors.
Published in: Bioorg Med Chem Lett
Target family: SLC12 family of cation-coupled chloride transporters (type: transporter)
Target: Basolateral Na-K-Cl symporter

Ligand: piretanide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.619999885559082 pIC50
Reference (Journal): Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
Published in: Naunyn Schmiedebergs Arch Pharmacol
Target family: SLC12 family of cation-coupled chloride transporters (type: transporter)
Target: Na-Cl symporter

Ligand: metolazone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  -

Ligand: hydrochlorothiazide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity:  -

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

Ligand: chlorothiazide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1958)
Primary target: yes
Median affinity:  -
Target family: SLC12 family of cation-coupled chloride transporters (type: transporter)
Target: Kidney-specific Na-K-Cl symporter

Ligand: piretanide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.96999979019165 pIC50
Reference (Journal): Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: furosemide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1966)
Primary target: yes
Median affinity: 5.150000095367432 pIC50
Reference (Journal): Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: bumetanide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1983)
Primary target: yes
Median affinity: 6.480000019073486 pIC50
Reference (Journal): Rat NKCC2/NKCC1 cotransporter selectivity for loop diuretic drugs.
Published in: Naunyn Schmiedebergs Arch Pharmacol
Target family: SLC12 family of cation-coupled chloride transporters (type: transporter)
Target: K-Cl cotransporter 4

Ligand: DIOA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -