upadacitinib
Upadacitinib 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. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
Ligand Summary
UNII: 4RA0KN46E0
PubChem: 58557659
Guide to Pharmacology: 9246
ChEMBL: CHEMBL3622821
DrugCentral: 5346
LyCHI: F9TLF4UV5U1J
Target Activities
JAK1
Tyrosine-protein kinase JAK1
5 Activities
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1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | |||||
IC50 | 7.37 | |||||
IC50 | 8.1 | MedChemComm, (2018) 9:3:477 | ||||
IC50 | 8.1 | Bioorg Med Chem, (2019) 27:12:2592 | ||||
IC50 | 7.33 | INHIBITOR | ||||
JAK2
Tyrosine-protein kinase JAK2
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.92 | |||||
IC50 | 8.1 | J Med Chem, (2018) 61:20:9030 | ||||
IC50 | 6.92 | INHIBITOR | ||||
JAK3
Tyrosine-protein kinase JAK3
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.64 | |||||
IC50 | 5.63 | INHIBITOR | ||||
TYK2
Non-receptor tyrosine-protein kinase TYK2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.33 | |||||