GYKI53784 [Ligand Id: 4210] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275006 (GYKI-52466) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| ChEMBL | Antagonist potency against functional AMPA receptor by kainate-induced Ca+2 in rat cerebellar granule neurons in primary culture | F | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1203-1205 [PMID:10866381] |
| ChEMBL | Ability to inhibit kainate-induced increase of calcium in rat cerebellar granule cells expressing AMPA receptor | F | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 167-170 [PMID:16216501] |
| ChEMBL | Displacement of [3H]CP-526427 from AMPA receptor in rat forebrain membranes | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 167-170 [PMID:16216501] |
| ChEMBL | Ability to displace [3H]CP-526427 from the AMPA receptor binding site in rat forebrain membranes | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 443-446 [PMID:12565947] |
| ChEMBL | Ability to displace [3H]CP-526427 (3 nM) from binding site of the Ionotropic glutamate receptor AMPA in rat forebrain membrane | B | 4.9 | pIC50 | 12600 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4427-4430 [PMID:14643339] |
| ChEMBL | Inhibitory activity against AMPA receptor currents in rat cortical cells stimulated with 50 uM kainic acid | F | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1996) 39: 343-346 [PMID:8558499] |
| ChEMBL | In vitro inhibition of AMPA receptor mediated currents in primary cultured rat fetal hippocampal neurons | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2005) 48: 4618-4627 [PMID:15999999] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Antagonist activity at open state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 3 mM glutamate by whole cell assay relative to control | B | 5.3 | pKi | 5000 | nM | Ki | Bioorg Med Chem (2017) 25: 3631-3637 [PMID:28571973] |
| ChEMBL | Antagonist activity at closed state of GFP-tagged GluA2Qflip isoform (unknown origin) expressed in HEK293S cells assessed as reduction in glutamate-induced current response in presence of 0.1 mM glutamate by whole cell assay | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem (2017) 25: 3631-3637 [PMID:28571973] |
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]
