DGIdb - CFTR Gene Record

CFTR 1080 Druggable Genome

Alternate Names:

1080
CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
CFTR
ABC35
ABCC7
CF
CFTR/MRP
MRP7
TNR-CFTR
dJ760C5.1
602421
1884
ENSG00000001626
OTTHUMG00000023076
707
P13569
cAMP-dependent chloride channel
Channel conductance-controlling ATPase
ATP-binding cassette sub-family C member 7
PA109
CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) (CAMP- DEPENDENT CHLORIDE CHANNEL). [SOURCE:UNIPROT/SWISSPROT;ACC:P13569]
BE0001195
CFTR_HUMAN
T55654
CF transmembrane conductance regulator

Gene Info:

GuideToPharmacology Gene Category Name	CFTR
GuideToPharmacology Gene Category ID	129
Target Class	Transporters
Target Subclass	TC:3.A.1.202.1
Human Readable Name	DRUGGABLE GENOME
Interpro Type	Domain
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	ABC TRANSPORTER
Interpro Acc	IPR001140
Uniprot Status	Swiss-Prot
Interpro Short Name	ABC_transptr_TM_dom
Interpro Name	ABC transporter, transmembrane domain
Gene Biotype	PROTEIN_CODING

(12 More Sources)

Gene Categories: Category Details

TRANSPORTER
CELL SURFACE
ION CHANNEL
ABC TRANSPORTER
DRUGGABLE GENOME

Publications:

Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem
Lubamba B et al., 2012, Cystic fibrosis: insight into CFTR pathophysiology and pharmacotherapy., Clin Biochem
Ikpa PT et al., 2014, Cystic fibrosis: toward personalized therapies., Int J Biochem Cell Biol
Awatade NT et al., 2014, Measurements of Functional Responses in Human Primary Lung Cells as a Basis for Personalized Therapy for Cystic Fibrosis., EBioMedicine
Compain P et al., 2013, Rescue of functional CFTR channels in cystic fibrosis: a dramatic multivalent effect using iminosugar cluster-based correctors., Chembiochem
Yu et al., 2012, Ivacaftor potentiation of multiple CFTR channels with gating mutations., J. Cyst. Fibros.
Kuk et al., 2015, Lumacaftor and ivacaftor in the management of patients with cystic fibrosis: current evidence and future prospects., Ther Adv Respir Dis
Boyle MP et al., 2014, A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial., Lancet Respir Med
Clancy JP et al., 2012, Results of a phase IIa study of VX-809, an investigational CFTR corrector compound, in subjects with cystic fibrosis homozygous for the F508del-CFTR mutation., Thorax
Norman P, 2014, Novel picolinamide-based cystic fibrosis transmembrane regulator modulators: evaluation of WO2013038373, WO2013038376, WO2013038381, WO2013038386 and WO2013038390., Expert Opin Ther Pat
Veit G et al., 2016, From CFTR biology toward combinatorial pharmacotherapy: expanded classification of cystic fibrosis mutations., Mol Biol Cell
Hubert D et al., 2017, Real-life initiation of lumacaftor/ivacaftor combination in adults with cystic fibrosis homozygous for the Phe508del CFTR mutation and severe lung disease., J Cyst Fibros
Kopeikin Z et al., 2014, Combined effects of VX-770 and VX-809 on several functional abnormalities of F508del-CFTR channels., J Cyst Fibros
Dekkers JF et al., 2016, Characterizing responses to CFTR-modulating drugs using rectal organoids derived from subjects with cystic fibrosis., Sci Transl Med
Van Goor F et al., 2011, Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809., Proc Natl Acad Sci U S A
Van Goor F et al., 2014, Effect of ivacaftor on CFTR forms with missense mutations associated with defects in protein processing or function., J Cyst Fibros
Fohner AE et al., 2017, PharmGKB summary: ivacaftor pathway, pharmacokinetics/pharmacodynamics., Pharmacogenet Genomics
Wang W et al., 2016, Robust Stimulation of W1282X-CFTR Channel Activity by a Combination of Allosteric Modulators., PLoS One
Tradtrantip et al., 2010, Crofelemer, an antisecretory antidiarrheal proanthocyanidin oligomer extracted from Croton lechleri, targets two distinct intestinal chloride channels., Mol. Pharmacol.
Arora K et al., 2016, Personalized medicine in cystic fibrosis: genistein supplementation as a treatment option for patients with a rare S1045Y-CFTR mutation., Am J Physiol Lung Cell Mol Physiol
Derand et al., 2002, The cystic fibrosis mutation G551D alters the non-Michaelis-Menten behavior of the cystic fibrosis transmembrane conductance regulator (CFTR) channel and abolishes the inhibitory Genistein binding site., J. Biol. Chem.
Devor et al., 1998, Ibuprofen inhibits cystic fibrosis transmembrane conductance regulator-mediated Cl- secretion., J. Clin. Invest.
Kerem E et al., 2008, Effectiveness of PTC124 treatment of cystic fibrosis caused by nonsense mutations: a prospective phase II trial., Lancet
Wilschanski M et al., 2011, Chronic ataluren (PTC124) treatment of nonsense mutation cystic fibrosis., Eur Respir J
Shoseyov D et al., 2016, Ataluren for the treatment of cystic fibrosis., Expert Rev Respir Med
Sermet-Gaudelus I et al., 2010, Ataluren (PTC124) induces cystic fibrosis transmembrane conductance regulator protein expression and activity in children with nonsense mutation cystic fibrosis., Am J Respir Crit Care Med
Tosco A et al., 2016, A novel treatment of cystic fibrosis acting on-target: cysteamine plus epigallocatechin gallate for the autophagy-dependent rescue of class II-mutated CFTR., Cell Death Differ
Donaldson SH et al., 2018, Tezacaftor/Ivacaftor in Subjects with Cystic Fibrosis and F508del/F508del-CFTR or F508del/G551D-CFTR., Am J Respir Crit Care Med
Saint-Criq V et al., 2017, Role of CFTR in epithelial physiology., Cell Mol Life Sci
Rowe SM et al., 2017, Tezacaftor-Ivacaftor in Residual-Function Heterozygotes with Cystic Fibrosis., N Engl J Med
Taylor-Cousar JL et al., 2017, Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del., N Engl J Med
Reddy et al., 1999, Bumetanide blocks CFTR GCl in the native sweat duct., Am. J. Physiol.
Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol
Zhou et al., 2002, Probing an open CFTR pore with organic anion blockers., J. Gen. Physiol.
Reddy et al., 2002, Effect of anion transport blockers on CFTR in the human sweat duct., J. Membr. Biol.
Jiang et al., 2003, Pleural surface fluorescence measurement of Na+ and Cl- transport across the air space-capillary barrier., J. Appl. Physiol.
Larsen et al., 2003, Beta-adrenergic receptors couple to CFTR chloride channels of intercalated mitochondria-rich cells in the heterocellular toad skin epithelium., Biochim. Biophys. Acta
Lee et al., 2005, Inhibition of Na+-K+ pump and L-type Ca2+ channel by glibenclamide in Guinea pig ventricular myocytes., J. Pharmacol. Exp. Ther.
Berger AL et al., 2005, Normal gating of CFTR requires ATP binding to both nucleotide-binding domains and hydrolysis at the second nucleotide-binding domain., Proc Natl Acad Sci U S A
Ramesh Babu PB et al., 2004, Regulation of apical surface fluid and protein secretion in human airway epithelial cell line Calu-3., Biochem Biophys Res Commun
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Sommer D et al., 2007, CFTR-dependent Cl- secretion in Xenopus laevis lung epithelium., Respir Physiol Neurobiol

LUMACAFTOR CFTR

Interaction Score: 45.44

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name VX-809

Novel drug target Established target

Trial Name VX-809 + VX-770

PMIDs:
26041577 22698459 24561283 26137539 24038832 22293084 26416827 24973281 21825083 24392786 26823392 28325531 24796242 27334259 21976485 23891399

Sources:
DTC FDA PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

TEZACAFTOR CFTR

Interaction Score: 18.94

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator positive modulator

Direct Interaction yes

Details of the Assay for Interaction Measuring the increase in cAMP/genistein-dependent current amplitude via the ΔF508-CFTR mutant expressed in NIH/3T3 cells by patch-clamp recording, in response to tezacaftor exposure.

PMIDs:
28930490 27714410 29099333 29099344

Sources:
FDA PharmGKB TTD DrugBank GuideToPharmacology ChemblInteractions

IVACAFTOR CFTR

Interaction Score: 7.57

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name VX-809 + VX-770

Novel drug target Established target

Trial Name VX-770

PMIDs:
27636560 22293084

Sources:
FDA TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
ELEXACAFTOR CFTR

Interaction Score: 5.68

Interaction Types & Directionality:

modulator

Interaction Info:

Specific Action of the Ligand Binding

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
FDA DrugBank GuideToPharmacology
CROFELEMER CFTR

Interaction Score: 5.68

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator inhibitor

Direct Interaction yes

Trial Name crofelemer

PMIDs:
19808995

Sources:
TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
ATALUREN CFTR

Interaction Score: 3.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18722008 21233271 26840186 20622033

Sources:
PharmGKB
GALICAFTOR CFTR

Interaction Score: 1.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BAMOCAFTOR CFTR

Interaction Score: 1.89

Interaction Types & Directionality:

n/a

Interaction Info:

Specific Action of the Ligand Binding

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IOWH-032 CFTR

Interaction Score: 1.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
QBW251 CFTR

Interaction Score: 1.89

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator activator

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL177991 CFTR

Interaction Score: 0.95

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CYSTEAMINE CFTR

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27035618

Sources:
PharmGKB
LONIDAMINE CFTR

Interaction Score: 0.76

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17490919

Sources:
DrugBank
GLYBURIDE CFTR

Interaction Score: 0.58

Interaction Types & Directionality:

antagonist (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
12407077 12202948 12391048 14729151 15365090

Sources:
DrugBank GuideToPharmacology
COLFORSIN CFTR

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15194485

Sources:
DrugBank
SCRIPTAID CFTR

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19966789

Sources:
DTC
DEXFOSFOSERINE CFTR

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
DEXIBUPROFEN CFTR

Interaction Score: 0.29

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9710435

Sources:
DrugBank
BUMETANIDE CFTR

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9886939

Sources:
DrugBank
ENTINOSTAT CFTR

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19966789

Sources:
DTC
TRICHOSTATIN CFTR

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19966789

Sources:
DTC
GENISTEIN CFTR

Interaction Score: 0.15

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
27261451 12124395

Sources:
NCI PharmGKB GuideToPharmacology
CAPSAICIN CFTR

Interaction Score: 0.11

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
FELODIPINE CFTR

Interaction Score: 0.09

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
IBUPROFEN CFTR

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
9710435

Sources:
DrugBank
NIMODIPINE CFTR

Interaction Score: 0.09

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Potentiation

PMIDs:
None found

Sources:
GuideToPharmacology
VORINOSTAT CFTR

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19966789

Sources:
DTC
APIGENIN CFTR

Interaction Score: 0.07

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ADENOSINE TRIPHOSPHATE CFTR

Interaction Score: 0.07

Interaction Types & Directionality:

cofactor (activating)

Interaction Info:

PMIDs:
15623556

Sources:
DrugBank
CURCUMIN CFTR

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27007499

Sources:
PharmGKB

Ensembl: ENSG00000001626
- Version: 101_38
Alternate Names:

CFTR Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P13569
- Version: 11-September-2012
Alternate Names:

CFTR Uniprot Gene Name

CFTR_HUMAN Uniprot Id

1080 Entrez Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Interpro Type Domain

Uniprot Evidence 1: Evidence at protein level

Gene Categories:

ABC TRANSPORTER, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P13569
- Version: January-2014
Alternate Names:

CFTR Gene Symbol

Gene Info:

Target Class Transporters

Target Subclass TC:3.A.1.202.1

Publications:

RussLampel: ENSG00000001626

Version: 26-July-2011

Alternate Names:

ENSG00000001626 Ensembl Gene Id

CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) (CAMP- DEPENDENT CHLORIDE CHANNEL). [SOURCE:UNIPROT/SWISSPROT;ACC:P13569] Description

CFTR Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

GuideToPharmacology: 1080
- Version: 29-September-2020
Alternate Names:

1884 HUGO Gene ID

1884 HUGO Gene Symbol

CF transmembrane conductance regulator HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name CFTR

GuideToPharmacology Gene Category ID 129

Gene Categories:

ION CHANNEL

Publications:

PharmGKB: CFTR

Version: 18-August-2020

Alternate Names:

PA109 PharmGKB ID

Gene Info:

Publications:

Carlile GW et al., 2016, Latonduine Analogs Restore F508del-Cystic Fibrosis Transmembrane Conductance Regulator Trafficking through the Modulation of Poly-ADP Ribose Polymerase 3 and Poly-ADP Ribose Polymerase 16 Activity., Mol Pharmacol

Boyle MP et al., 2014, A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial., Lancet Respir Med

Taylor-Cousar JL et al., 2018, Lumacaftor/ivacaftor in patients with cystic fibrosis and advanced lung disease homozygous for F508del-CFTR., J Cyst Fibros

DrugBank: BE0001195

Version: 5.1.7

Alternate Names:

CFTR DrugBank Gene Name

P13569 UniProt Accession

1080 Entrez Gene Id

Gene Info:

Publications:

Reddy et al., 1999, Bumetanide blocks CFTR GCl in the native sweat duct., Am. J. Physiol.

Zhou et al., 2002, Probing an open CFTR pore with organic anion blockers., J. Gen. Physiol.

Reddy et al., 2002, Effect of anion transport blockers on CFTR in the human sweat duct., J. Membr. Biol.

NCI: CFTR

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Saeed et al., 2008, Fenretinide prevents the development of osteoporosis in Cftr-KO mice., J. Cyst. Fibros.

Derand et al., 2002, The cystic fibrosis mutation G551D alters the non-Michaelis-Menten behavior of the cystic fibrosis transmembrane conductance regulator (CFTR) channel and abolishes the inhibitory Genistein binding site., J. Biol. Chem.

DTC: CFTR

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Hutt DM et al., 2010, Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis., Nat Chem Biol

Pesce E et al., 2015, Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis., Eur J Med Chem

HingoraniCasas: ENSG00000001626
- Version: 31-May-2017
Alternate Names:

ENSG00000001626 Gene Symbol

CFTR Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ABCC7
- Version: chembl_23
Alternate Names:

ABCC7 GENE_SYMBOL

CFTR GENE_SYMBOL

Cystic fibrosis transmembrane conductance regulator UNIPROT

Gene Info:

Publications:
Pharos: CFTR
- Version: 03-September-2020
Alternate Names:

Cystic fibrosis transmembrane conductance regulator Gene Name

P13569 UniProt ID

Gene Info:

Gene Categories:

TRANSPORTER, ION CHANNEL

Publications:
GO: CFTR
- Version: 05-September-2020
Alternate Names:

ABCC7 GO Gene Synonym

Gene Info:

Gene Categories:

CELL SURFACE, ABC TRANSPORTER

Publications:
Tempus: CFTR
- Version: 11-November-2018
Alternate Names:

CFTR Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
TTD: cAMP-dependent chloride channel
- Version: 2020.06.01
Alternate Names:

CFTR TTD Gene Abbreviation

T55654 TTD Target ID

Gene Info:

Publications:
FDA: CFTR
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:

Trial Name	VX-809
Novel drug target	Established target
Trial Name	VX-809 + VX-770

Mechanism of Interaction	Cystic fibrosis transmembrane conductance regulator positive modulator
Direct Interaction	yes
Details of the Assay for Interaction	Measuring the increase in cAMP/genistein-dependent current amplitude via the ΔF508-CFTR mutant expressed in NIH/3T3 cells by patch-clamp recording, in response to tezacaftor exposure.

Specific Action of the Ligand	Binding
Endogenous Drug?	False
Direct Interaction?	False

Specific Action of the Ligand	Potentiation
Endogenous Drug?	False

ENSG00000001626	Ensembl Gene Id
CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) (CAMP- DEPENDENT CHLORIDE CHANNEL). [SOURCE:UNIPROT/SWISSPROT;ACC:P13569]	Description
CFTR	Display Id

1884	HUGO Gene ID
1884	HUGO Gene Symbol
CF transmembrane conductance regulator	HUGO Gene Name

CFTR	DrugBank Gene Name
P13569	UniProt Accession
1080	Entrez Gene Id

ABCC7	GENE_SYMBOL
CFTR	GENE_SYMBOL
Cystic fibrosis transmembrane conductance regulator	UNIPROT

Cystic fibrosis transmembrane conductance regulator	Gene Name
P13569	UniProt ID

antagonist (inhibitory)
inhibitor (inhibitory)

antagonist (inhibitory)
blocker (inhibitory)

CFTR Gene Record

CFTR 1080 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: modulator

Interaction Info: Trial Name VX-809 Novel drug target Established target Trial Name VX-809 + VX-770

PMIDs: 26041577 22698459 24561283 26137539 24038832 22293084 26416827 24973281 21825083 24392786 26823392 28325531 24796242 27334259 21976485 23891399

Sources: DTC FDA PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: activator (activating)

PMIDs: 28930490 27714410 29099333 29099344

Sources: FDA PharmGKB TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: activator (activating) potentiator

Interaction Info: Trial Name VX-809 + VX-770 Novel drug target Established target Trial Name VX-770

PMIDs: 27636560 22293084

Sources: FDA TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: modulator

Interaction Info: Specific Action of the Ligand Binding Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: FDA DrugBank GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator inhibitor Direct Interaction yes Trial Name crofelemer

PMIDs: 19808995

Sources: TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18722008 21233271 26840186 20622033

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: Specific Action of the Ligand Binding Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: activator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator activator

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Specific Action of the Ligand Potentiation Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27035618

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17490919

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory) blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False

PMIDs: 12407077 12202948 12391048 14729151 15365090

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 15194485

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19966789

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 9710435

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 9886939

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name VX-809

Novel drug target Established target

Trial Name VX-809 + VX-770

PMIDs:
26041577 22698459 24561283 26137539 24038832 22293084 26416827 24973281 21825083 24392786 26823392 28325531 24796242 27334259 21976485 23891399

Sources:
DTC FDA PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

activator (activating)

PMIDs:
28930490 27714410 29099333 29099344

Sources:
FDA PharmGKB TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

activator (activating)

potentiator

Interaction Info:

Trial Name VX-809 + VX-770

Novel drug target Established target

Trial Name VX-770

PMIDs:
27636560 22293084

Sources:
FDA TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

modulator

Interaction Info:

Specific Action of the Ligand Binding

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
FDA DrugBank GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator inhibitor

Direct Interaction yes

Trial Name crofelemer

PMIDs:
19808995

Sources:
TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
18722008 21233271 26840186 20622033

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Specific Action of the Ligand Binding

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Cystic fibrosis transmembrane conductance regulator activator

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
27035618

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
17490919

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
12407077 12202948 12391048 14729151 15365090

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
15194485

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
19966789

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
9710435

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
9886939

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
19966789

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19966789

Sources:
DTC

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
27261451 12124395

Sources:
NCI PharmGKB GuideToPharmacology

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

activator (activating)