(S)-5-fluorowillardiine [Ligand Id: 4070] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL123132 (5-Fluorowillardiine, (S)-5-Fluorowillardiine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 1 expressed in HEK293 cells | B | 7.83 | pKi | 14.7 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| ChEMBL | Agonist activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes | F | 6.42 | pEC50 | 382 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA1 receptor expressed in Xenopus oocytes | F | 6.42 | pEC50 | 380 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR1 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262] | ||||||||
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells | B | 7.6 | pKi | 25.1 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| ChEMBL | Agonist activity at recombinant GluA2 receptor flip isoform expressed in Xenopus oocytes | F | 6.33 | pEC50 | 463 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA2/Glutamate receptor ionotropic, AMPA 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3503] [GtoPdb: 445] [UniProtKB: P19491] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR2(R) expressed in Sf9 cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR2(Q) expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 6.34 | pEC50 | 460 | 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] | ||||||||
| ChEMBL | Agonist activity at recombinant GluA3 receptor expressed in Xenopus oocytes | F | 4.68 | pEC50 | 20900 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| ChEMBL | Agonist activity at recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes | F | 4.68 | pEC50 | 20900 | nM | EC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
| GluA3/Glutamate receptor ionotropic, AMPA 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3504] [GtoPdb: 446] [UniProtKB: P19492] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 expressed in Sf9 cells | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR3 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 4.68 | pEC50 | 20900 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058] | ||||||||
| ChEMBL | Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 expressed in HEK293 cells | B | 6.52 | pKi | 305 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
| GluA4/Glutamate receptor ionotropic, AMPA 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493] | ||||||||
| ChEMBL | Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR4 expressed in Sf9 cells | B | 6.91 | pKi | 123 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| ChEMBL | Agonist activity at cyclothiazide-desensitized rat recombinant flip iGluR4 expressed in Xenopus laevis oocytes by two electrode voltage-clamp electrophysiology method | F | 4.92 | pEC50 | 11900 | nM | EC50 | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
| ChEMBL | Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells | B | 5.86 | pKi | 1380 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluK2/Glutamate receptor ionotropic kainate 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3607] [GtoPdb: 451] [UniProtKB: P42260] | ||||||||
| ChEMBL | Displacement of [3H]kainic acid from rat recombinant iGluR6(V,C,R) receptor expressed in Sf9 cells | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2008) 51: 6614-6618 [PMID:18811139] |
| GluK5/Glutamate receptor ionotropic kainate 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2675] [GtoPdb: 454] [UniProtKB: Q16478] | ||||||||
| ChEMBL | Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 expressed in HEK293 cells | B | 5.74 | pKi | 1820 | nM | Ki | J Med Chem (1997) 40: 3645-3650 [PMID:9357531] |
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]
