Pharos : Ligand Details - tofacitinib

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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

Ligand Structure

Rendered image for the query structure

Synonyms & Links

UNII: 87LA6FU830

PubChem: 9926791

Guide to Pharmacology: 5677

ChEMBL: CHEMBL221959

DrugCentral: 4713

LyCHI: MP4M7KJWPRGV

Target Activities

Explore Associated and Predicted Targets

JAK3

Tclin

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			24417533

IC50	8.22			27572962

Kd	9.8		Nat. Biotechnol., (2011) 29:11:1046	22037378

Ki	9.62		J. Med. Chem., (2012) 55:12:5901	22591402

IC50	9.62		J Med Chem, (2018) 61:23:10440	30460842

IC50	9.54		J Med Chem, (2018) 61:12:5350	29852068

IC50	9.47		J Med Chem, (2017) 60:23:9676	29156136

IC50	9.46		Bioorg. Med. Chem. Lett., (2016) 26:7:1803	26927423

Ki	9.4		J. Med. Chem., (2012) 55:12:5901	22591402

Ki	9.4		J. Med. Chem., (2013) 56:11:4764	23659214

JAK2

Tclin

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			24417533

IC50	9.3		Bioorg Med Chem, (2019) 27:8:1646	30853331

Kd	9.24		Nat. Biotechnol., (2011) 29:11:1046	22037378

IC50	9.22		J. Med. Chem., (2014) 57:22:9323	25369270

Ki	9.15		J. Med. Chem., (2012) 55:12:5901	22591402

Ki	9.15		J. Med. Chem., (2013) 56:11:4764	23659214

Ki	9.15		J. Med. Chem., (2013) 56:11:4521	23668484

Ki	9		J. Med. Chem., (2012) 55:12:5901	22591402

IC50	9		Bioorg Med Chem, (2019) 27:12:2592	30926315

IC50	8.96		J Med Chem, (2018) 61:23:10440	30460842

JAK1

Tclin

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)
Ki	7.82			24417533

IC50	9.3		J Med Chem, (2018) 61:12:5350	29852068

Ki	9.17		J. Med. Chem., (2012) 55:12:5901	22591402

Ki	9.15		J. Med. Chem., (2012) 55:12:5901	22591402

Ki	9.15		J. Med. Chem., (2013) 56:11:4764	23659214

Ki	9.15		J. Med. Chem., (2013) 56:11:4521	23668484

IC50	9.1		J. Med. Chem., (2014) 57:22:9323	25369270

IC50	8.89		Bioorg. Med. Chem. Lett., (2016) 26:7:1803	26927423

IC50	8.89		J Med Chem, (2017) 60:23:9676	29156136

IC50	8.89		J Med Chem, (2020) 63:6:2915	32134643

TYK2

Tclin

Non-receptor tyrosine-protein kinase TYK2

14 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.31			24417533

IC50	8.44		Bioorg. Med. Chem., (2014) 22:3:1156	24398382

Ki	8.36		J. Med. Chem., (2012) 55:12:5901	22591402

Kd	8.32		Nat. Biotechnol., (2011) 29:11:1046	22037378

Ki	8.14		J. Med. Chem., (2013) 56:11:4764	23659214

Ki	8.11		J. Med. Chem., (2012) 55:12:5901	22591402

Ki	8.11		J. Med. Chem., (2013) 56:11:4521	23668484

IC50	8.05		J Med Chem, (2018) 61:12:5350	29852068

IC50	7.98		J Med Chem, (2018) 61:23:10440	30460842

IC50	7.92		J Med Chem, (2017) 60:23:9676	29156136

DCLK3

Tchem

Serine/threonine-protein kinase DCLK3

4 Activities

Items per page:

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	19053756

Kd	8.35		Nat. Biotechnol., (2008) 26:1:127	18183025

Kd	7.92		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.35		https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL221959

PKN1

Tchem

Serine/threonine-protein kinase N1

1 Activities

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1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.91			27572962