flupirtine [Ligand Id: 2598] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL255044 (Flupirtine, Flupirtinte, W-2964) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Serine hydroxymethyltransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295747] [UniProtKB: P34897] | ||||||||
| ChEMBL | Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay | B | 6.03 | pIC50 | 933.25 | nM | IC50 | WO-2016085990-A1. Compositions and methods relating to inhibiting serine hyrdoxymethyltransferase 2 activity (null) |
| Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221348] [GtoPdb: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
| GtoPdb | - | - | 5 | pEC50 | - | - | - | J Neurosci (2004) 24: 592-7 [PMID:14736843] |
| ChEMBL | Agonist activity at human KCNQ2/3 expressed in HEK293 cells by FLIPR based thallium influx assay | B | 6.25 | pEC50 | 560 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 126603-126603 [PMID:31416667] |
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]
