cyclothiazide [Ligand Id: 4167] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL61593 (35483, Anhydron, Cyclothiazide, Fluidil, NSC-758431) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluA1/GluA2/Glutamate receptor AMPA 1/2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883294] [GtoPdb: 444, 445] [UniProtKB: P42261, P42262] | ||||||||
| ChEMBL | Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current | B | 4.12 | pEC50 | >76000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GtoPdb | - | - | 4.72 | pEC50 | 19000 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| ChEMBL | Activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as effect on 300 uM glutamate-induced current | B | 5.18 | pEC50 | 6600 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GtoPdb | - | - | 5.65 | pEC50 | 2240 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| GluA1/GluA2/GluA3/GluA4 in Human [GtoPdb: 444, 445, 446, 447] [UniProtKB: P42261, P42262, P42263, P48058] | ||||||||
| GtoPdb | - | - | 4.72 | pEC50 | 19000 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| GtoPdb | - | - | 4.86 | pEC50 | 13700 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| GtoPdb | - | - | 5.41 | pEC50 | 3910 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| GtoPdb | - | - | 5.65 | pEC50 | 2240 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| 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 | Inhibition of binding to AMPA receptor from rat cerebral cortex | B | 5.21 | pIC50 | 6100 | nM | IC50 | J Med Chem (2001) 44: 302-304 [PMID:11462971] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
| ChEMBL | Activity at human recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | B | 4.7 | pEC50 | 19800 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GtoPdb | - | - | 4.72 | pEC50 | 19000 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| ChEMBL | Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay | B | 5 | pEC50 | 10000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay | B | 5.7 | pEC50 | 2000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Activity at human recombinant GluA2 receptor flop isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | B | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at human GluA2(Q)i expressed in HEK293 cells assessed as enhancement of glutamate-evoked desensitized current by whole cell patch clamp method | B | 5.12 | pEC50 | 7600 | nM | EC50 | J Med Chem (2016) 59: 448-461 [PMID:26653877] |
| ChEMBL | Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | B | 5.65 | pEC50 | 2240 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GtoPdb | - | - | 5.65 | pEC50 | 2240 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
| ChEMBL | Agonist activity at rat flip iGluR2(Q) expressed in Xenopus laevis oocytes by whole cell patch-clamp method | F | 5.12 | pEC50 | 7600 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
| GtoPdb | - | - | 4.86 | pEC50 | 13700 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| ChEMBL | Activity at human recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay | B | 4.86 | pEC50 | 13700 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
| GtoPdb | - | - | 5.41 | pEC50 | 3910 | nM | EC50 | Neuropharmacology (2001) 40: 976-83 [PMID:11406188] |
| ChEMBL | Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells | F | 5.42 | pEC50 | 3800 | nM | EC50 | J Med Chem (2000) 43: 4354-4358 [PMID:11087558] |
| ChEMBL | Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | F | 5.42 | pEC50 | 3800 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5057-5061 [PMID:16879964] |
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]
