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

chemical structure image

Synonyms & Links

UNII: 87LA6FU830

PubChem: 9926791

Guide to Pharmacology: 5677

ChEMBL: CHEMBL221959

DrugCentral: 4713

LyCHI: MP4M7KJWPRGV

Target Activities

JAK3

Tclin

Tyrosine-protein kinase JAK3

33 Activities

Items per page:

1 – 10 of 33

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.62		J. Med. Chem., (2011) 54:1:284	21155605

IC50	7.89		Bioorg. Med. Chem. Lett., (2006) 16:21:5633	16934457

IC50	7.89		Bioorg. Med. Chem. Lett., (2007) 17:5:1250	17189692

IC50	7.96		Bioorg. Med. Chem., (2014) 22:3:1156	24398382

IC50	8.1		J. Med. Chem., (2011) 54:1:284	21155605

IC50	8.3		Bioorg. Med. Chem. Lett., (2009) 19:20:5887	19762238

IC50	8.4		Bioorg. Med. Chem. Lett., (2016) 26:12:2936	27130359

IC50	8.48		J. Med. Chem., (2010) 53:24:8468	21105711

IC50	8.49		J. Med. Chem., (2010) 53:24:8468	21105711

Kd	8.66		Bioorg. Med. Chem. Lett., (2010) 20:24:7454	21106455

JAK2

Tclin

Tyrosine-protein kinase JAK2

30 Activities

Items per page:

1 – 10 of 30

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.7		J. Med. Chem., (2008) 51:24:8012	19053756

IC50	7.7		Science, (2003) 302:5646:875	14593182

IC50	7.92		J. Med. Chem., (2011) 54:1:284	21155605

IC50	7.96		Bioorg. Med. Chem. Lett., (2006) 16:21:5633	16934457

IC50	7.96		Bioorg. Med. Chem. Lett., (2007) 17:5:1250	17189692

IC50	7.97		Bioorg. Med. Chem. Lett., (2014) 24:4:1116	24461299

Kd	8.3		Bioorg. Med. Chem. Lett., (2010) 20:24:7454	21106455

Kd	8.3		Nat. Biotechnol., (2008) 26:1:127	18183025

IC50	8.39		J. Med. Chem., (2014) 57:12:5023	24417533

IC50	8.4		J. Med. Chem., (2011) 54:24:8440	22087750

JAK1

Tclin

Tyrosine-protein kinase JAK1

26 Activities

Items per page:

1 – 10 of 26

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.58		J. Med. Chem., (2011) 54:24:8440	22087750

IC50	7.82		J. Med. Chem., (2014) 57:12:5023	24417533

IC50	7.82		Bioorg. Med. Chem., (2016) 24:12:2660	27137359

IC50	8.21		J. Med. Chem., (2011) 54:1:284	21155605

IC50	8.39		J. Med. Chem., (2010) 53:24:8468	21105711

IC50	8.42		Bioorg. Med. Chem. Lett., (2014) 24:4:1116	24461299

IC50	8.43		Bioorg. Med. Chem., (2015) 23:15:4846	26059596

IC50	8.48		Bioorg. Med. Chem., (2014) 22:3:1156	24398382

IC50	8.49		J. Med. Chem., (2014) 57:12:5023	24417533

IC50	8.52		J. Med. Chem., (2011) 54:24:8440	22087750

TYK2

Tclin

Non-receptor tyrosine-protein kinase TYK2

11 Activities

Items per page:

1 – 10 of 11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.62		Bioorg. Med. Chem. Lett., (2014) 24:4:1116	24461299

IC50	7.89		Bioorg. Med. Chem. Lett., (2016) 26:7:1803	26927423

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

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

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

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

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

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

IC50	6.30999994			24417533

IC50	6.64	INHIBITOR	https://www.ebi.ac.uk/chembl/compound/inspect/CHEMBL221959

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

Kd	8.35		J. Med. Chem., (2008) 51:24:8012	19053756

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

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

PKN1

Tchem

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)
IC50	6.90999985			27572962