Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T47941 Target Info
Target Name Phosphodiesterase 4 (PDE4)
Synonyms
PDE-4
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class Phosphoric diester hydrolase
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name Opioid receptor sigma 1 (OPRS1) Successful Target
UniProt ID SGMR1_HUMAN
Gene Name SIGMAR1
Synonyms
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) SUN13834 Drug Info Ki = 0.83 nM [1]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) SUN13834 Drug Info Ki = 170 nM [2]
Co-Target Name Adenosine A1 receptor (ADORA1) Successful Target
UniProt ID AA1R_HUMAN
Gene Name ADORA1
Synonyms
Adenosine receptor A1; A(1) adenosine receptor
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Representative Drug(s) Roflumilast Drug Info IC50 ~ 1000 nM [3]
Co-Target Name Adenosine A2a receptor (ADORA2A) Successful Target
UniProt ID AA2AR_HUMAN
Gene Name ADORA2A
Synonyms
Adenosine receptor A2a; ADORA2; A2a Adenosine receptor; A(2A) adenosine receptor
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Representative Drug(s) Roflumilast Drug Info IC50 ~ 1000 nM [3]
Co-Target Name Adenosine A2b receptor (ADORA2B) Successful Target
UniProt ID AA2BR_HUMAN
Gene Name ADORA2B
Synonyms
Adenosine receptor A2b; A2b Adenosine receptor
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Representative Drug(s) Roflumilast Drug Info IC50 ~ 1000 nM [3]
Co-Target Name Cholestenol delta-isomerase (EBP) Clinical trial Target
UniProt ID EBP_HUMAN
Gene Name EBP
Synonyms
Emopamilbinding protein; EBP; Delta(8)Delta(7) sterol isomerase; D8D7 sterol isomerase; 3betahydroxysteroidDelta(8),Delta(7)isomerase
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Representative Drug(s) SUN13834 Drug Info Ki = 165 nM [1]
Co-Target Name Phosphodiesterase 7A (PDE7A) Discontinued Target
UniProt ID PDE7A_HUMAN
Gene Name PDE7A
Synonyms
TM22; High affinity cAMPspecific 3',5'cyclic phosphodiesterase 7A; High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A
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Representative Drug(s) crisaborole Drug Info IC50 = 730 nM [4]
References  Top
REF 1 Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. J Med Chem. 2005 Jul 28;48(15):4754-64.
REF 2 Development of a pharmacophore for inhibition of human liver cytochrome P-450 2D6: molecular modeling and inhibition studies. J Med Chem. 1993 Apr 30;36(9):1136-45.
REF 3 Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships. J Med Chem. 2016 Dec 8;59(23):10479-97.
REF 4 Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2129-32.

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