baricitinib
Baricitinib is a selective and reversible inhibitor of Janus kinase (JAK)1 and JAK2. Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in haematopoiesis, inflammation and immune function. Within the intracellular signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signalling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs. FDA issued an Emergency use authorization (EUA) on November 19, 2020 that permits use of baricitinib in combination with remdesivir for treatment of suspected or laboratory-confirmed COVID-19 in hospitalized patients ≥2 years of age requiring supplemental oxygen, invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO).
Ligand Summary
UNII: ISP4442I3Y
PubChem: 44205240
Guide to Pharmacology: 7792
ChEMBL: CHEMBL2105759
DrugCentral: 5202
LyCHI: ZVWX826G5X2B
Target Activities
JAK1
Tyrosine-protein kinase JAK1
10 Activities
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1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.4 | |||||
IC50 | 8.23 | |||||
IC50 | 9 | J. Med. Chem., (2016) 59:2:733 | ||||
IC50 | 8.4 | J. Med. Chem., (2014) 57:12:5023 | ||||
IC50 | 8.4 | Bioorg. Med. Chem., (2016) 24:12:2660 | ||||
IC50 | 8.4 | J Med Chem, (2018) 61:3:1130 | ||||
IC50 | 8.23 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 8.23 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 8.22 | J. Med. Chem., (2015) 58:18:7596 | ||||
IC50 | 8.23 | INHIBITOR | ||||
JAK2
Tyrosine-protein kinase JAK2
10 Activities
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1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 8.24 | |||||
IC50 | 8.15 | |||||
IC50 | 9.1 | J. Med. Chem., (2016) 59:2:733 | ||||
IC50 | 8.24 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 8.24 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 8.22 | J. Med. Chem., (2015) 58:18:7596 | ||||
IC50 | 8.18 | J. Med. Chem., (2014) 57:12:5023 | ||||
IC50 | 8.15 | Bioorg. Med. Chem., (2016) 24:12:2660 | ||||
IC50 | 8.15 | J Med Chem, (2018) 61:3:1130 | ||||
IC50 | 8.24 | INHIBITOR | ||||
JAK3
Tyrosine-protein kinase JAK3
2 Activities
TYK2
Non-receptor tyrosine-protein kinase TYK2
2 Activities
SEPT9
Septin-9
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 7.08 | Science, (2017) 358:6367:None | ||||
Q6ZSR9
Uncharacterized protein FLJ45252
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Kd | 7.11 | Science, (2017) 358:6367:None | ||||
AAK1
AP2-associated protein kinase 1
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
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Kd | 7.77 | INHIBITOR | ||||