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 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]
