tofacitinib
Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
Ligand Summary
UNII: 87LA6FU830
PubChem: 9926791
Guide to Pharmacology: 5677
ChEMBL: CHEMBL221959
DrugCentral: 4713
LyCHI: MP4M7KJWPRGV
Target Activities
JAK3
Tyrosine-protein kinase JAK3
48 Activities
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1 – 10 of 48
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.26 | |||||
IC50 | 8.22 | |||||
Kd | 9.8 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 9.62 | J. Med. Chem., (2012) 55:12:5901 | ||||
IC50 | 9.62 | J Med Chem, (2018) 61:23:10440 | ||||
IC50 | 9.54 | J Med Chem, (2018) 61:12:5350 | ||||
IC50 | 9.47 | J Med Chem, (2017) 60:23:9676 | ||||
IC50 | 9.46 | Bioorg. Med. Chem. Lett., (2016) 26:7:1803 | ||||
Ki | 9.4 | J. Med. Chem., (2012) 55:12:5901 | ||||
Ki | 9.4 | J. Med. Chem., (2013) 56:11:4764 | ||||
JAK2
Tyrosine-protein kinase JAK2
44 Activities
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1 – 10 of 44
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.11 | |||||
IC50 | 9.3 | Bioorg Med Chem, (2019) 27:8:1646 | ||||
Kd | 9.24 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
IC50 | 9.22 | J. Med. Chem., (2014) 57:22:9323 | ||||
Ki | 9.15 | J. Med. Chem., (2012) 55:12:5901 | ||||
Ki | 9.15 | J. Med. Chem., (2013) 56:11:4764 | ||||
Ki | 9.15 | J. Med. Chem., (2013) 56:11:4521 | ||||
Ki | 9 | J. Med. Chem., (2012) 55:12:5901 | ||||
IC50 | 9 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 8.96 | J Med Chem, (2018) 61:23:10440 | ||||
JAK1
Tyrosine-protein kinase JAK1
42 Activities
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1 – 10 of 42
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Ki | 7.82 | |||||
IC50 | 9.3 | J Med Chem, (2018) 61:12:5350 | ||||
Ki | 9.17 | J. Med. Chem., (2012) 55:12:5901 | ||||
Ki | 9.15 | J. Med. Chem., (2012) 55:12:5901 | ||||
Ki | 9.15 | J. Med. Chem., (2013) 56:11:4764 | ||||
Ki | 9.15 | J. Med. Chem., (2013) 56:11:4521 | ||||
IC50 | 9.1 | J. Med. Chem., (2014) 57:22:9323 | ||||
IC50 | 8.89 | Bioorg. Med. Chem. Lett., (2016) 26:7:1803 | ||||
IC50 | 8.89 | J Med Chem, (2017) 60:23:9676 | ||||
IC50 | 8.89 | J Med Chem, (2020) 63:6:2915 | ||||
TYK2
Non-receptor tyrosine-protein kinase TYK2
14 Activities
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1 – 10 of 14
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.31 | |||||
IC50 | 8.44 | Bioorg. Med. Chem., (2014) 22:3:1156 | ||||
Ki | 8.36 | J. Med. Chem., (2012) 55:12:5901 | ||||
Kd | 8.32 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Ki | 8.14 | J. Med. Chem., (2013) 56:11:4764 | ||||
Ki | 8.11 | J. Med. Chem., (2012) 55:12:5901 | ||||
Ki | 8.11 | J. Med. Chem., (2013) 56:11:4521 | ||||
IC50 | 8.05 | J Med Chem, (2018) 61:12:5350 | ||||
IC50 | 7.98 | J Med Chem, (2018) 61:23:10440 | ||||
IC50 | 7.92 | J Med Chem, (2017) 60:23:9676 | ||||
DCLK3
Serine/threonine-protein kinase DCLK3
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Kd | 8.35 | J. Med. Chem., (2008) 51:24:8012 | ||||
Kd | 8.35 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.92 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.35 | |||||
PKN1
Serine/threonine-protein kinase N1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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IC50 | 6.91 | |||||