An EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor that specifically blocks the action of phosphodiesterase IV.
| Member | Definition | Class |
|---|
| an2728 | A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults. | crisaborole |
| apremilast | A member of the class of isoindoles that is isoindole-1,3-dione substituted at position 4 by an acetamido group and at position 1 by a 1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl group. Used for treatment of psoriatic arthritis. | apremilast |
| etazolate | A pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties. | etazolate |
| roflumilast | A benzamide obtained by formal condensation of the carboxy group of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid with the amino group of 3,5-dichloropyridin-4-amine. Used for treatment of bronchial asthma and chronic obstructive pulmonary disease. | roflumilast |
| rp 73401 | A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 3-(cyclopentyloxy)-4-methoxybenzoic acid with the primary amino group of 3,5-dichloropyridin-4-amine. | piclamilast |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|
| 3',5'-cyclic-AMP phosphodiesterase | Sus scrofa (pig) | IC50 | 0.0010 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Adenosine receptor A2a | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Adenosine receptor A2b | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0010 | 1 | 1 |
| Beta-lactamase | Klebsiella pneumoniae | IC50 | 0.6700 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A | Homo sapiens (human) | IC50 | 2,803.0500 | 2 | 2 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Homo sapiens (human) | IC50 | 929.0429 | 2 | 21 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Homo sapiens (human) | IC50 | 71,000.0000 | 1 | 1 |
| Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | Homo sapiens (human) | IC50 | 4,724.2810 | 2 | 21 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Homo sapiens (human) | IC50 | 0.0469 | 27 | 31 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Homo sapiens (human) | Ki | 0.0011 | 6 | 6 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4A | Rattus norvegicus (Norway rat) | Ki | 0.0260 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | IC50 | 19.7928 | 57 | 85 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | Ki | 0.0010 | 7 | 7 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Rattus norvegicus (Norway rat) | Ki | 0.0260 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Homo sapiens (human) | IC50 | 0.0506 | 25 | 29 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Homo sapiens (human) | Ki | 0.0011 | 6 | 6 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4C | Rattus norvegicus (Norway rat) | Ki | 0.0260 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | IC50 | 22.1083 | 43 | 73 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | Ki | 0.0011 | 6 | 6 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Rattus norvegicus (Norway rat) | Ki | 0.0260 | 1 | 1 |
| cAMP-specific 3',5'-cyclic phosphodiesterase 7B | Homo sapiens (human) | IC50 | 80.4951 | 1 | 20 |
| Carboxylic ester hydrolase | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| cGMP-dependent 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 249.5191 | 2 | 21 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | IC50 | 21,368.8000 | 3 | 3 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | IC50 | 2,746.1955 | 3 | 22 |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase B | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 2,748.0906 | 2 | 21 |
| Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | IC50 | 0.0006 | 1 | 29 |
| Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4D | Homo sapiens (human) | IC50 | 0.0019 | 1 | 22 |
| Chain A, cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 0.0004 | 1 | 8 |
| Chain B, cAMP-specific 3',5'-cyclic phosphodiesterase 4B | Homo sapiens (human) | IC50 | 0.0004 | 1 | 4 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A | Homo sapiens (human) | IC50 | 80.4951 | 1 | 20 |
| Endothelin-1 receptor | Sus scrofa (pig) | IC50 | 0.0010 | 1 | 1 |
| High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A | Homo sapiens (human) | IC50 | 1,015.3650 | 2 | 2 |
| High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A | Homo sapiens (human) | IC50 | 80.4951 | 1 | 20 |
| Phosphodiesterase | Trypanosoma brucei | Ki | 3.1623 | 1 | 1 |
| Sodium-dependent serotonin transporter | Rattus norvegicus (Norway rat) | IC50 | 0.5002 | 2 | 2 |