UBP302 [Ligand Id: 4333] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL372797 (UBP-302) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
| ChEMBL | Displacement of [3H]S-glutamate from rat GluR5 S1S2 ligand binding core expressed in Escherichia coli (DE3) | B | 5.4 | pKd | 3940 | nM | Kd | Bioorg Med Chem (2009) 17: 6390-6401 [PMID:19656686] |
| ChEMBL | Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers | F | 6.4 | pKd | 402 | nM | Kd | J Med Chem (2005) 48: 7867-7881 [PMID:16302825] |
| ChEMBL | Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres | F | 6.4 | pKd | 402 | nM | Kd | J Med Chem (2007) 50: 1558-1570 [PMID:17348638] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003] | ||||||||
| ChEMBL | Antagonist activity at recombinant GluK3 receptor (unknown origin) expressed in Xenopus oocyte assessed as inhibition of glutamate-induced current amplitude by voltage-clamp method | B | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5568-5572 [PMID:27765511] |
| GluK5/Glutamate receptor ionotropic kainate 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4041] [GtoPdb: 454] [UniProtKB: Q63273] | ||||||||
| ChEMBL | Antagonist activity against GLUK5-containing kainate receptor by inhibition of kainate-induced depolarization of neonatal rat dorsal root fibers | F | 6.4 | pKd | 402 | nM | Kd | J Med Chem (2006) 49: 2579-2592 [PMID:16610801] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
