Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T76414 | Target Info | |||
| Target Name | Glutamate receptor ionotropic NMDA 2B (NMDAR2B) | ||||
| 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
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| Target Type | Successful Target | ||||
| Gene Name | GRIN2B | ||||
| Biochemical Class | Glutamate-gated ion channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | Alpha 1-PI | Drug Info | IC50 = 3.9 nM | [1] | ||
| 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
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| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 = 100 nM | [2] | ||
| Co-Target Name | Glutamate receptor AMPA 2 (GRIA2) | Successful Target | ||||
| UniProt ID | GRIA2_HUMAN | |||||
| Gene Name | GRIA2 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 2; Glutamate receptor 2; GluRK2; GluRB; GluR2; GluR-K2; GluR-B; GluR-2; GluA2; AMPAselective glutamate receptor 2; AMPA-selective glutamate receptor 2
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| Representative Drug(s) | NBQX | Drug Info | Ki = 210 nM | [3] | ||
| Co-Target Name | Glutamate receptor AMPA 4 (GRIA4) | Successful Target | ||||
| UniProt ID | GRIA4_HUMAN | |||||
| Gene Name | GRIA4 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 4; GluRD; GluR4; GluA4; GRIA4; AMPAselective glutamate receptor 4
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| Representative Drug(s) | NBQX | Drug Info | Ki = 600 nM | [4] | ||
| Co-Target Name | Glutamate receptor AMPA 3 (GRIA3) | Successful Target | ||||
| UniProt ID | GRIA3_HUMAN | |||||
| Gene Name | GRIA3 | |||||
| Synonyms |
Glutamate receptor ionotropic, AMPA 3; GluRK3; GluRC; GluR3; GluA3; GRIA3; AMPAselective glutamate receptor 3
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| Representative Drug(s) | NBQX | Drug Info | Ki = 900 nM | [4] | ||
| Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
| UniProt ID | DRD2_HUMAN | |||||
| Gene Name | DRD2 | |||||
| Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
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| 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
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| 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
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| Representative Drug(s) | Alpha 1-PI | Drug Info | IC50 ~ 1000 nM | [1] | ||
| Co-Target Name | Glutamate receptor ionotropic (GRI) | Clinical trial Target | ||||
| UniProt ID | GRIA1_HUMAN; GRIA2_HUMAN; GRIA3_HUMAN; GRIA4_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | NBQX | Drug Info | IC50 = 52 nM | [5] | ||
| References | Top | ||||
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| 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 | 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 3 | Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. J Med Chem. 2005 Jun 30;48(13):4200-3. | ||||
| REF 4 | Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine. J Med Chem. 2002 Sep 26;45(20):4383-6. | ||||
| REF 5 | Homology modeling of the ampa receptor: A quantitative predictive tool for the design of novel antagonists. Bioorg Med Chem Lett. 1997 Jun 3;7(11):1437-42. | ||||
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