apremilast
Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined.
Ligand Summary
UNII: UP7QBP99PN
PubChem: 11561674
Guide to Pharmacology: 7372
ChEMBL: CHEMBL514800
DrugCentral: 4829
LyCHI: GTQW8KGMM25B
Target Activities
PDE4D
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
7 Activities
Items per page:
1 – 7 of 7
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.48 | |||||
IC50 | 7.48 | Eur J Med Chem, (2019) 174:None:198 | ||||
IC50 | 7.46 | J Med Chem, (2019) 62:10:4884 | ||||
IC50 | 7.32 | J Nat Prod, (2020) 83:4:1229 | ||||
IC50 | 7.13 | J Med Chem, (2019) 62:11:5579 | ||||
IC50 | 6.27 | J Med Chem, (2020) 63:6:3370 | ||||
IC50 | 7.13 | INHIBITOR | ||||
PDE4B
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
3 Activities
PDE4A
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.85 | |||||
PDE4C
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.93 | |||||