Target family: CFTR (type: other_ic)
Target: CFTR

Ligand: CFTRinh-172 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: CBIQ (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: compound 16d [PMID: 36573286] (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pEC50
Reference (Journal): Synthetic Strategies for Improving Solubility: Optimization of Novel Pyrazolo[1,5-<i>a</i>]pyrimidine CFTR Activator That Ameliorates Dry Eye Disease.
Published in: J Med Chem

Ligand: crofelemer (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012)
Primary target: yes
Median affinity: 5.150000095367432 pIC50
Reference (Journal): Crofelemer, an antisecretory antidiarrheal proanthocyanidin oligomer extracted from Croton lechleri, targets two distinct intestinal chloride channels.
Published in: Mol Pharmacol

Ligand: elexacaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.150000095367432 pEC50
Reference (Patent): Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Ligand: elexacaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 7.150000095367432 pEC50
Reference (Journal): VX-445-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles.
Published in: N Engl J Med

Ligand: lumacaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2015)
Primary target: no
Median affinity: 5.590000152587891 pEC50
Reference (Journal): Novel Hits in the Correction of ΔF508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.
Published in: J Med Chem

Ligand: ivacaftor (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: yes
Approval source: FDA and EMA (2012)
Median affinity:  -

Ligand: ivacaftor (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity:  -
Reference (Journal): CFTR function, pathology and pharmacology at single-molecule resolution.
Published in: Nature

Ligand: icenticaftor (Synthetic organic)
Interaction type: None
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pEC50
Reference (Journal): Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Published in: J Med Chem

Ligand: GlyH-101 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: GLPG2737 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pEC50
Reference (Journal): Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
Published in: J Med Chem

Ligand: GLPG2737 (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.159999847412109 pEC50
Reference (Journal): Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
Published in: J Med Chem

Ligand: GLPG1837 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): GLPG1837, a CFTR potentiator, in p.Gly551Asp (G551D)-CF patients: An open-label, single-arm, phase 2a study (SAPHIRA1).
Published in: J Cyst Fibros

Ligand: glibenclamide (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (as glyburide, 1984), EMA (2018)
Median affinity: 4.66 pKi
Reference (Journal): Effect of ATP-sensitive K+ channel regulators on cystic fibrosis transmembrane conductance regulator chloride currents.
Published in: J Gen Physiol

Ligand: genistein (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: GaTx1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: felodipine (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: yes
Approval source: FDA (1991)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Structure-activity relationship of 1,4-dihydropyridines as potentiators of the cystic fibrosis transmembrane conductance regulator chloride channel.
Published in: Mol Pharmacol

Ligand: UCCF-029 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: tezacaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2018)
Primary target: no
Median affinity: 6.570000171661377 pEC50
Reference (Patent): Indole derivatives as CFTR modulators.

Ligand: sulfonamide-01 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: phenylglycine-01 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: NS004 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: nimodipine (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: yes
Approval source: FDA (1988)
Median affinity:  -

Ligand: ABBV-3221 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): CFTR function, pathology and pharmacology at single-molecule resolution.
Published in: Nature

Ligand: ABBV-3221 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.
Published in: ACS Med Chem Lett

Ligand: apigenin (Natural product)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: bamocaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pEC50
Reference (Journal): VX-659-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles.
Published in: N Engl J Med

Ligand: UCCF-853 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: UCCF-339 (Synthetic organic)
Interaction type: Activator
Action: Potentiation
Ligand approved: no
Median affinity:  -

Ligand: bamocaftor (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pEC50
Reference (Patent): Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator

Ligand: capsaicin (Natural product)
Interaction type: Activator
Action: Potentiation
Ligand approved: yes
Approval source: EMA & FDA (2009)
Median affinity:  -