DGIdb - TOFACITINIB Drug Record

TOFACITINIB chembl:CHEMBL221959 ApprovedImmunotherapy

Alternate Names:

CP-690
550
CP-690,550 FREE BASE
CP-690550 FREE BASE
CP690550
CP-690-550
CP- 690 550
CP 690550
CP-690,550
CP-690550
TASOCITINIB
CP690,550
TOFACITINIB
XELJANZ®
rxcui:1357536
chemidplus:477600-75-2
drugbank:08895
pubchem.compound:9926791
chembl:CHEMBL221959

Drug Info:

(2 More Sources)

Publications:

Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem
Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science
Jang WD et al., 2015, Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design., Bioorg Med Chem Lett
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem
Hou S et al., 2014, Novel carbazole inhibits phospho-STAT3 through induction of protein-tyrosine phosphatase PTPN6., J Med Chem
Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov
Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood
Yin et al., 2015, Identification of mutant alleles of JAK3 in pediatric patients with acute lymphoblastic leukemia., Leuk. Lymphoma
Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.
Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

TOFACITINIB STAT5A

Interaction Score: 10.63

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19053756 14593182

Sources:
DTC
TOFACITINIB STAT5B

Interaction Score: 4.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14593182

Sources:
DTC
TOFACITINIB PTPN6

Interaction Score: 3.54

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24978112

Sources:
DTC
TOFACITINIB PKN1

Interaction Score: 2.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
TOFACITINIB JAK3

Interaction Score: 1.77

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources:
DTC JAX-CKB CIViC GuideToPharmacology TTD
TOFACITINIB TYK2

Interaction Score: 0.91

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26231159 10592235

Sources:
DTC GuideToPharmacology
TOFACITINIB JAK1

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical enzyme assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
10592235

Sources:
GuideToPharmacology
TOFACITINIB JAK2

Interaction Score: 0.39

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26258521 10592235

Sources:
DTC GuideToPharmacology
TOFACITINIB YES1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DTC: TOFACITINIB

Version: 02-September-2020

Alternate Names:

CHEMBL221959 ChEMBL Drug ID

Drug Info:

Publications:

Changelian PS et al., 2003, Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor., Science

Jiang JK et al., 2008, Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)., J Med Chem

Tan L et al., 2015, Development of Selective Covalent Janus Kinase 3 Inhibitors., J Med Chem

JAX-CKB: Tofacitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Losdyck et al., 2015, Distinct Acute Lymphoblastic Leukemia (ALL)-associated Janus Kinase 3 (JAK3) Mutants Exhibit Different Cytokine-Receptor Requirements and JAK Inhibitor Specificities., J. Biol. Chem.

Koo et al., 2012, Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma., Cancer Discov

Elliott et al., 2011, FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma., Blood

CIViC: TOFACITINIB
- Version: 14-September-2020
Alternate Names:

Drug Info:

Publications:

Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood
GuideToPharmacology: 178102304
- Version: 29-September-2020
Alternate Names:

TOFACITINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Tofacitinib
- Version: 2020.06.01
Alternate Names:

D0EG1I TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL221959
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

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

Details of the Assay for Interaction	In a biochemical enzyme assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

antagonist (inhibitory)
inhibitor (inhibitory)

TOFACITINIB Drug Record

TOFACITINIB chembl:CHEMBL221959 ApprovedImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19053756 14593182

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14593182

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24978112

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources: DTC JAX-CKB CIViC GuideToPharmacology TTD

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: 26231159 10592235

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Details of the Assay for Interaction In a biochemical enzyme assay. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 10592235

Sources: GuideToPharmacology

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

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

PMIDs: 26258521 10592235

Sources: DTC GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DTC: TOFACITINIB

Alternate Names: CHEMBL221959 ChEMBL Drug ID

Drug Info:

JAX-CKB: Tofacitinib

Alternate Names:

Drug Info:

CIViC: TOFACITINIB

Alternate Names:

Drug Info:

Publications: Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

GuideToPharmacology: 178102304

Alternate Names: TOFACITINIB GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Tofacitinib

Alternate Names: D0EG1I TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL221959

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
19053756 14593182

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
14593182

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
24978112

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
14593182 26258521 22705984 21821710 25146434 26446793 25193870 10592235

Sources:
DTC JAX-CKB CIViC GuideToPharmacology TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26231159 10592235

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction In a biochemical enzyme assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
10592235

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
26258521 10592235

Sources:
DTC GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

CHEMBL221959 ChEMBL Drug ID

Publications:

Degryse et al., 2014, JAK3 mutants transform hematopoietic cells through JAK1 activation, causing T-cell acute lymphoblastic leukemia in a mouse model., Blood

Alternate Names:

TOFACITINIB GuideToPharmacology Ligand Name

Alternate Names:

D0EG1I TTD Drug ID