Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T22839 | Target Info | |||
| Target Name | Pancreatic elastase 1 (CELA1) | ||||
| Synonyms |
Elastase; CELA1
Click to Show/Hide
|
||||
| Target Type | Successful Target | ||||
| Gene Name | CELA1 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| 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
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 = 3.9 nM | [1] | ||
| Co-Target Name | Glutamate receptor ionotropic NMDA 2B (NMDAR2B) | Successful Target | ||||
| UniProt ID | NMDE2_HUMAN | |||||
| Gene Name | GRIN2B | |||||
| Synonyms |
NR3; NR2B; NMDA receptor subunit 2B; NMDA receptor NR2B; NMDA NR2B receptor; N-methylD-aspartate receptor subtype 2B; N-methyl-D-aspartate receptor subunit 3; N-methyl D-aspartate receptor subtype 2B; HNR3; Glutamate receptor ionotropic, NMDA 2B; Glutamate receptor NR2B subunit; Glutamate [NMDA] receptor subunit epsilon-2; GluN2B
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | Ki = 10 nM | [2] | ||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 = 100 nM | [3] | ||
| Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
| UniProt ID | DRD2_HUMAN | |||||
| Gene Name | DRD2 | |||||
| Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 ~ 1000 nM | [1] | ||
| Co-Target Name | Histamine H1 receptor (H1R) | Successful Target | ||||
| UniProt ID | HRH1_HUMAN | |||||
| Gene Name | HRH1 | |||||
| Synonyms |
HH1R; H1R
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 = 1000 nM | [1] | ||
| Co-Target Name | Opioid receptor mu (MOP) | Successful Target | ||||
| UniProt ID | OPRM_HUMAN | |||||
| Gene Name | OPRM1 | |||||
| Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
Click to Show/Hide
|
|||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 ~ 1000 nM | [1] | ||
| Co-Target Name | Neutrophil elastase (NE) | Clinical trial Target | ||||
| UniProt ID | ELNE_HUMAN | |||||
| Gene Name | ELANE | |||||
| Synonyms |
PMN elastase; Medullasin; Human leukocyte elastase; HLE; Elastase-2; ELA2; Bone marrow serine protease
Click to Show/Hide
|
|||||
| Representative Drug(s) | Sivelestat | Drug Info | IC50 = 10 nM | [4] | ||
| Co-Target Name | Leukocyte proteinase-3 (PRTN3) | Clinical trial Target | ||||
| UniProt ID | PRTN3_HUMAN | |||||
| Gene Name | PRTN3 | |||||
| Synonyms |
Wegener autoantigen; PR3; PR-3; P29; Neutrophil proteinase 4; NP4; NP-4; Myeloblastin; MBN; Leukocyte proteinase 3; CANCA antigen; C-ANCA antigen; AGP7
Click to Show/Hide
|
|||||
| Representative Drug(s) | Sivelestat | Drug Info | IC50 = 340 nM | [5] | ||
| Co-Target Name | Glutamate NMDA receptor GRIN1/GRIN2B (GRIN1/GRIN2B) | Co-Target | ||||
| UniProt ID | NMDZ1_HUMAN-NMDE2_HUMAN | |||||
| Gene Name | GRIN1-GRIN2B | |||||
| Representative Drug(s) | Alpha 1-PI | Drug Info | Ki = 10 nM | [6] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds. J Med Chem. 1991 Oct;34(10):3085-90. | ||||
| REF 2 | Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines. Bioorg Med Chem. 2014 Dec 1;22(23):6638-46. | ||||
| REF 3 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
| REF 4 | Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors. J Med Chem. 2013 Dec 12;56(23):9802-6. | ||||
| REF 5 | Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3. Bioorg Med Chem. 2015 Mar 1;23(5):1123-34. | ||||
| REF 6 | Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold. Eur J Med Chem. 2018 Sep 5;157:397-404. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.