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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
