Target Information
| Target General Information | Top | |||||
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| Target ID |
T76414
(Former ID: TTDC00299)
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| Target Name |
Glutamate receptor ionotropic NMDA 2B (NMDAR2B)
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| 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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| Gene Name |
GRIN2B
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Alpha-1-antitrypsin deficiency [ICD-11: 5C5A] | |||||
| Function |
Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+). Sensitivity to glutamate and channel kinetics depend on the subunit composition. In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an irreversible neuronal death. Contributes to neural pattern formation in the developing brain. Plays a role in long-term depression (LTD) of hippocampus membrane currents and in synaptic plasticity. Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium.
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| BioChemical Class |
Glutamate-gated ion channel
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| UniProt ID | ||||||
| Sequence |
MKPRAECCSPKFWLVLAVLAVSGSRARSQKSPPSIGIAVILVGTSDEVAIKDAHEKDDFH
HLSVVPRVELVAMNETDPKSIITRICDLMSDRKIQGVVFADDTDQEAIAQILDFISAQTL TPILGIHGGSSMIMADKDESSMFFQFGPSIEQQASVMLNIMEEYDWYIFSIVTTYFPGYQ DFVNKIRSTIENSFVGWELEEVLLLDMSLDDGDSKIQNQLKKLQSPIILLYCTKEEATYI FEVANSVGLTGYGYTWIVPSLVAGDTDTVPAEFPTGLISVSYDEWDYGLPARVRDGIAII TTAASDMLSEHSFIPEPKSSCYNTHEKRIYQSNMLNRYLINVTFEGRNLSFSEDGYQMHP KLVIILLNKERKWERVGKWKDKSLQMKYYVWPRMCPETEEQEDDHLSIVTLEEAPFVIVE SVDPLSGTCMRNTVPCQKRIVTENKTDEEPGYIKKCCKGFCIDILKKISKSVKFTYDLYL VTNGKHGKKINGTWNGMIGEVVMKRAYMAVGSLTINEERSEVVDFSVPFIETGISVMVSR SNGTVSPSAFLEPFSADVWVMMFVMLLIVSAVAVFVFEYFSPVGYNRCLADGREPGGPSF TIGKAIWLLWGLVFNNSVPVQNPKGTTSKIMVSVWAFFAVIFLASYTANLAAFMIQEEYV DQVSGLSDKKFQRPNDFSPPFRFGTVPNGSTERNIRNNYAEMHAYMGKFNQRGVDDALLS LKTGKLDAFIYDAAVLNYMAGRDEGCKLVTIGSGKVFASTGYGIAIQKDSGWKRQVDLAI LQLFGDGEMEELEALWLTGICHNEKNEVMSSQLDIDNMAGVFYMLGAAMALSLITFICEH LFYWQFRHCFMGVCSGKPGMVFSISRGIYSCIHGVAIEERQSVMNSPTATMNNTHSNILR LLRTAKNMANLSGVNGSPQSALDFIRRESSVYDISEHRRSFTHSDCKSYNNPPCEENLFS DYISEVERTFGNLQLKDSNVYQDHYHHHHRPHSIGSASSIDGLYDCDNPPFTTQSRSISK KPLDIGLPSSKHSQLSDLYGKFSFKSDRYSGHDDLIRSDVSDISTHTVTYGNIEGNAAKR RKQQYKDSLKKRPASAKSRREFDEIELAYRRRPPRSPDHKRYFRDKEGLRDFYLDQFRTK ENSPHWEHVDLTDIYKERSDDFKRDSVSGGGPCTNRSHIKHGTGDKHGVVSGVPAPWEKN LTNVEWEDRSGGNFCRSCPSKLHNYSTTVTGQNSGRQACIRCEACKKAGNLYDISEDNSL QELDQPAAPVAVTSNASTTKYPQSPTNSKAQKKNRNKLRRQHSYDTFVDLQKEEAALAPR SVSLKDKGRFMDGSPYAHMFEMSAGESTFANNKSSVPTAGHHHHNNPGGGYMLSKSLYPD RVTQNPFIPTFGDDQCLLHGSKSYFFRQPTVAGASKARPDFRALVTNKPVVSALHGAVPA RFQKDICIGNQSNPCVPNNKNPRAFNGSSNGHVYEKLSSIESDV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T18RS6 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Alpha 1-PI | Drug Info | Approved | Alpha-1 antitrypsin deficiency | [2], [3] | |
| Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
| 1 | CERC-301 | Drug Info | Phase 2 | Major depressive disorder | [5] | |
| 2 | CP-101,606 | Drug Info | Phase 2 | Parkinson disease | [6] | |
| 3 | ELIPRODIL | Drug Info | Phase 2 | Multiple sclerosis | [7] | |
| 4 | RGH-896 | Drug Info | Phase 2 | Peripheral neuropathy | [8] | |
| 5 | EVT100 | Drug Info | Phase 1 | Major depressive disorder | [9] | |
| 6 | NBQX | Drug Info | Phase 1 | Neurological disorder | [10] | |
| 7 | Neu-2000 | Drug Info | Phase 1 | Cardiac arrest | [11] | |
| Discontinued Drug(s) | [+] 10 Discontinued Drugs | + | ||||
| 1 | EVT-101 | Drug Info | Discontinued in Phase 2 | Neuropathic pain | [12] | |
| 2 | YM-90K | Drug Info | Discontinued in Phase 2 | Convulsion | [13] | |
| 3 | Besonprodil | Drug Info | Discontinued in Phase 1 | Parkinson disease | [14] | |
| 4 | EVT-103 | Drug Info | Discontinued in Phase 1 | Major depressive disorder | [15] | |
| 5 | DIZOCILPINE | Drug Info | Terminated | Cerebrovascular ischaemia | [16], [17] | |
| 6 | L-689560 | Drug Info | Terminated | Neurodegenerative disorder | [18], [19] | |
| 7 | L-698532 | Drug Info | Terminated | Neurological disorder | [20] | |
| 8 | L-698544 | Drug Info | Terminated | Alzheimer disease | [21] | |
| 9 | L-701324 | Drug Info | Terminated | Cerebrovascular ischaemia | [22], [23], [24] | |
| 10 | RO-25-6981 | Drug Info | Terminated | Cancer related pain | [25] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Antagonist | [+] 26 Antagonist drugs | + | ||||
| 1 | Alpha 1-PI | Drug Info | [1] | |||
| 2 | CERC-301 | Drug Info | [26] | |||
| 3 | CP-101,606 | Drug Info | [27] | |||
| 4 | RGH-896 | Drug Info | [8] | |||
| 5 | EVT100 | Drug Info | [9] | |||
| 6 | Neu-2000 | Drug Info | [30] | |||
| 7 | EVT-101 | Drug Info | [31] | |||
| 8 | Besonprodil | Drug Info | [31] | |||
| 9 | EVT-103 | Drug Info | [33] | |||
| 10 | L-689560 | Drug Info | [35] | |||
| 11 | RO-25-6981 | Drug Info | [38] | |||
| 12 | CGP61594 | Drug Info | [35] | |||
| 13 | Conantokins G | Drug Info | [57] | |||
| 14 | Conantokins T | Drug Info | [57] | |||
| 15 | d-AP5 | Drug Info | [35] | |||
| 16 | d-CCPene | Drug Info | [35] | |||
| 17 | LY233053 | Drug Info | [35] | |||
| 18 | NP93-31 | Drug Info | [35] | |||
| 19 | NVP-AAM077 | Drug Info | [64] | |||
| 20 | Ro 63-1908 | Drug Info | [66] | |||
| 21 | Tenocyclidine | Drug Info | [67] | |||
| 22 | UBP141 | Drug Info | [41] | |||
| 23 | [3H]CGP39653 | Drug Info | [35] | |||
| 24 | [3H]CGS19755 | Drug Info | [35] | |||
| 25 | [3H]CPP | Drug Info | [35] | |||
| 26 | [3H]MDL105519 | Drug Info | [35] | |||
| Inhibitor | [+] 77 Inhibitor drugs | + | ||||
| 1 | ELIPRODIL | Drug Info | [28] | |||
| 2 | NBQX | Drug Info | [29] | |||
| 3 | YM-90K | Drug Info | [32] | |||
| 4 | DIZOCILPINE | Drug Info | [34] | |||
| 5 | L-695902 | Drug Info | [36] | |||
| 6 | L-698532 | Drug Info | [37] | |||
| 7 | L-698544 | Drug Info | [36] | |||
| 8 | L-701324 | Drug Info | [37] | |||
| 9 | RPR-104632 | Drug Info | [39] | |||
| 10 | (D)-Ala-Pro-Glu | Drug Info | [40] | |||
| 11 | (R)-2-Amino-5-phosphono-pentanoic acid | Drug Info | [41] | |||
| 12 | (R)-2-Amino-7-phosphono-heptanoic acid | Drug Info | [41] | |||
| 13 | 1,3-ditolylguanidine | Drug Info | [42] | |||
| 14 | 2-(4-benzyl-piperidin-1-ylmethyl)-1H-indol-6-ol | Drug Info | [43] | |||
| 15 | 2-(4-Phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [44] | |||
| 16 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-4-ol | Drug Info | [44] | |||
| 17 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ol | Drug Info | [44] | |||
| 18 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ylamine | Drug Info | [44] | |||
| 19 | 2-Methylamino-succinic acid(NMDA) | Drug Info | [35], [45] | |||
| 20 | 2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [46] | |||
| 21 | 3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one | Drug Info | [36] | |||
| 22 | 3-Hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 23 | 3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 24 | 3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 25 | 3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 26 | 4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [48] | |||
| 27 | 4,6-Dichloro-1H-indole-2-carboxylic acid | Drug Info | [49] | |||
| 28 | 4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline | Drug Info | [46] | |||
| 29 | 4-Benzyl-1-(2-phenoxy-ethyl)-piperidine | Drug Info | [28] | |||
| 30 | 4-Benzyl-1-phenethyl-piperidine hydrochloride | Drug Info | [50] | |||
| 31 | 4-Bromo-3-hydroxy-1H-quinolin-2-one | Drug Info | [48] | |||
| 32 | 4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [48] | |||
| 33 | 4-Chloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [48] | |||
| 34 | 4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one | Drug Info | [37] | |||
| 35 | 4-[2-(3-Phenyl-propylamino)-ethyl]-phenol | Drug Info | [50] | |||
| 36 | 4-[2-(4-Benzyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | [28] | |||
| 37 | 4-[2-(4-Phenyl-butoxy)-ethyl]-phenol | Drug Info | [50] | |||
| 38 | 4-[2-(4-Phenyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | [28] | |||
| 39 | 4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol | Drug Info | [50] | |||
| 40 | 4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol | Drug Info | [50] | |||
| 41 | 4-[3-(4-Phenyl-butylamino)-propyl]-phenol | Drug Info | [51] | |||
| 42 | 4-[3-(5-Phenyl-pentylamino)-propyl]-phenol | Drug Info | [50] | |||
| 43 | 5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | [52] | |||
| 44 | 5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one | Drug Info | [36] | |||
| 45 | 5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [36] | |||
| 46 | 6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | [52] | |||
| 47 | 6-Chloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [53] | |||
| 48 | 6-Methoxy-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [44] | |||
| 49 | 6-Nitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [53] | |||
| 50 | 6-Nitro-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [44] | |||
| 51 | 7-chloro-3-hydroxyquinazoline-2,4-dione | Drug Info | [54] | |||
| 52 | 8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 53 | 8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 54 | 8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [47] | |||
| 55 | Ala-Pro-Glu | Drug Info | [40] | |||
| 56 | AP-7 | Drug Info | [55] | |||
| 57 | Conantokin-G | Drug Info | [56] | |||
| 58 | DNQX | Drug Info | [58] | |||
| 59 | Gly-Amp-Glu | Drug Info | [40] | |||
| 60 | Gly-Hyp-Glu | Drug Info | [40] | |||
| 61 | Gly-Pip-Glu | Drug Info | [40] | |||
| 62 | H-Gly-D-dmP-Glu-OH | Drug Info | [60] | |||
| 63 | H-Gly-dmP-Glu-OH | Drug Info | [60] | |||
| 64 | N,N'-Bis-(4-butoxy-phenyl)-guanidine | Drug Info | [42] | |||
| 65 | N,N'-Bis-(4-butyl-phenyl)-guanidine | Drug Info | [42] | |||
| 66 | N,N'-Bis-(4-ethyl-phenyl)-guanidine | Drug Info | [42] | |||
| 67 | N,N'-Bis-(4-isopropyl-phenyl)-guanidine | Drug Info | [42] | |||
| 68 | N-(2-methoxybenzyl)cinnamamidine | Drug Info | [61] | |||
| 69 | N-(3-phenethoxybenzyl)-4-hydroxybenzamide | Drug Info | [62] | |||
| 70 | N-(4-(benzyloxy)phenethyl)pyridin-4-amine | Drug Info | [63] | |||
| 71 | Nle-Pro-Glu | Drug Info | [40] | |||
| 72 | Phe-Pro-Glu | Drug Info | [40] | |||
| 73 | PHENCYCLIDINE | Drug Info | [65] | |||
| 74 | Phenethyl-(3-phenyl-propyl)-amine | Drug Info | [50] | |||
| 75 | Phenethyl-(4-phenyl-butyl)-amine | Drug Info | [50] | |||
| 76 | RPR-118723 | Drug Info | [39] | |||
| 77 | TRANSTORINE | Drug Info | [49] | |||
| Agonist | [+] 5 Agonist drugs | + | ||||
| 1 | (+)-HA966 | Drug Info | [35] | |||
| 2 | (RS)-(tetrazol-5-yl)glycine | Drug Info | [35] | |||
| 3 | D-aspartic acid | Drug Info | [35] | |||
| 4 | homoquinolinic acid | Drug Info | [35] | |||
| 5 | L-aspartic acid | Drug Info | [35] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | CN-2097 | Drug Info | [35] | |||
| Modulator (allosteric modulator) | [+] 1 Modulator (allosteric modulator) drugs | + | ||||
| 1 | DQP-1105 | Drug Info | [59] | |||
| Blocker (channel blocker) | [+] 2 Blocker (channel blocker) drugs | + | ||||
| 1 | N1-dansyl-spermine | Drug Info | [35] | |||
| 2 | [3H]dizocilpine | Drug Info | [35] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Adenosine triphosphate | Ligand Info | |||||
| Structure Description | Cocrystal structure of human CaMKII-alpha (CAMK2A)kinase domain and GluN2B(S1303D) | PDB:7KL1 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [68] |
| PDB Sequence |
RNKLRRQHDY
1304 DTFVD
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| Ligand Name: Esketamine | Ligand Info | |||||
| Structure Description | Structure of the human GluN1-GluN2B NMDA receptor in complex with S-ketamine,glycine and glutamate | PDB:7EU8 | ||||
| Method | Electron microscopy | Resolution | 4.07 Å | Mutation | No | [69] |
| PDB Sequence |
SIGIAVILVS
45 DEVAIKDAHE55 KDDFHHLSVV65 PRVELVAMNE75 TDPKSIITRI85 CDLMSDRKIQ 95 GVVFADDTDQ105 EAIAQILDFI115 SAQTLTPILG125 IHGGSSMIMA135 DKDESSMFFQ 145 FGPSIEQQAS155 VMLNIMEEYD165 WYIFSIVTTY175 FPGYQDFVNK185 IRSTIENSFV 195 GWELEDSKIQ217 NQLKKLQSPI227 ILLYCTKEEA237 TYIFEVANSV247 GLTGYGYTWI 257 VPSLVAGDTD267 TVPAEFPTGL277 ISVSYDEWDY287 GLPARVRDGI297 AIITTAASDM 307 LSEHSFIPEP317 KSSCYNTHEK327 QSNMLNRYLI340 NVTFEGRNLS350 FSEDGYQMHP 360 KLVIILLNKE370 RKWERVGKWK380 DKSLQMKYYV390 WPDDHLSIVT410 LEEAPFVIVE 420 SVDPLSGTCM430 RNTVPCQKRI440 VGYIKKCCKG459 FCIDILKKIS469 KSVKFTYDLY 479 LVTNGKHGKK489 INGTWNGMIG499 EVVMKRAYMA509 VGSLTINEER519 SEVVDFSVPF 529 IETGISVMVS539 RSNGTVSPSA549 FLEPFSADVW559 VMMFVMLLIV569 SAVAVFVFEY 579 FTIGKAIWLL609 WGLVFNNSVP619 VQNPKGTTSK629 IMVSVWAFFA639 VIFLASYTAN 649 LAAFMIQEEY659 VDQVSGLSDK669 KFQRPNDFSP679 PFRFGTVPNG689 STERNIRNNY 699 AEMHAYMGKF709 NQRGVDDALL719 SLKTGKLDAF729 IYDAAVLNYM739 AGRDEGCKLV 749 TIGSGKVFAS759 TGYGIAIQKD769 SGWKRQVDLA779 ILQLFGDGEM789 EELEALWLTG 799 ICHNSSQLDI815 DNMAGVFYML825 GAAMALSLIT835 FIC
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Ras signaling pathway | hsa04014 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Rap1 signaling pathway | hsa04015 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| cAMP signaling pathway | hsa04024 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Circadian entrainment | hsa04713 | Affiliated Target |
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| Class: Organismal Systems => Environmental adaptation | Pathway Hierarchy | ||
| Long-term potentiation | hsa04720 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Glutamatergic synapse | hsa04724 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Dopaminergic synapse | hsa04728 | Affiliated Target |
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| Class: Organismal Systems => Nervous system | Pathway Hierarchy | ||
| Click to Show/Hide the Information of Affiliated Human Pathways | |||
| Degree | 23 | Degree centrality | 2.47E-03 | Betweenness centrality | 1.72E-03 |
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| Closeness centrality | 2.40E-01 | Radiality | 1.42E+01 | Clustering coefficient | 1.26E-01 |
| Neighborhood connectivity | 3.07E+01 | Topological coefficient | 6.13E-02 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | NMDA receptor stimulation induces reversible fission of the neuronal endoplasmic reticulum. PLoS One. 2009;4(4):e5250. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003666) | |||||
| REF 4 | ClinicalTrials.gov (NCT04722666) Study of Efficacy and Safety of MIJ821 in Addition to Comprehensive Standard of Care on the Rapid Reduction of Symptoms of Major Depressive Disorder in Subjects Who Have Suicidal Ideation With Intent. U.S. National Institutes of Health. | |||||
| REF 5 | ClinicalTrials.gov (NCT02459236) A Study of Intermittent Doses of CERC-301 in MDD. | |||||
| REF 6 | ClinicalTrials.gov (NCT00073476) A Study to Evaluate the Efficacy and Safety of CP-101,606 in Subjects With an Acute Stroke. U.S. National Institutes of Health. | |||||
| REF 7 | ClinicalTrials.gov (NCT00001929) Treatment of Parkinson's Disease With Eliprodil. U.S. National Institutes of Health. | |||||
| REF 8 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
| REF 9 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
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