(12E,20Z,18S)-8-hydroxyvariabilin [Ligand Id: 4072] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL464651 ((12E,20Z,18S)-8-Hydroxyvariabilin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Dual specificity protein phosphatase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2635] [UniProtKB: P51452] | ||||||||
| ChEMBL | Inhibition of human VHR expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | B | 5.03 | pIC50 | 9400 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1159-1161 [PMID:28189419] |
| glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415] | ||||||||
| ChEMBL | Agonist activity at human recombinant alpha 1 GlyR expressed in HEK293 cells assessed as potentiation of glycine current by whole cell patch clamp assay | F | 5.92 | pEC50 | 1200 | nM | EC50 | Bioorg Med Chem (2010) 18: 2912-2919 [PMID:20346682] |
| glycine receptor α3 subunit/Glycine receptor subunit alpha-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075092] [GtoPdb: 425] [UniProtKB: O75311] | ||||||||
| ChEMBL | Antagonist activity at human recombinant alpha 3 GlyR expressed in HEK293 cells assessed as inhibition of glycine current influx by whole cell patch clamp assay | F | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2912-2919 [PMID:20346682] |
| GtoPdb | - | - | 5.2 | pIC50 | 7000 | nM | IC50 | |
| RTP Type C/Leukocyte common antigen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3243] [GtoPdb: 1852] [UniProtKB: P08575] | ||||||||
| ChEMBL | Inhibition of human CD45 cytoplasmic domain (584 to 1281 residues) expressed in yeast using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1159-1161 [PMID:28189419] |
| protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031] | ||||||||
| ChEMBL | Inhibition of recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | B | 5.15 | pIC50 | 7100 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1159-1161 [PMID:28189419] |
| protein tyrosine phosphatase non-receptor type 2/T-cell protein-tyrosine phosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3807] [GtoPdb: 3255] [UniProtKB: P17706] | ||||||||
| ChEMBL | Inhibition of full length recombinant N-terminal GST-tagged human TCPTP expressed in Escherichia coli using pNPP as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins | B | 5.43 | pIC50 | 3700 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1159-1161 [PMID:28189419] |
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]
