(R)-NFPS [Ligand Id: 4618] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL180966 (ALX-5407) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GAL1 receptor/Galanin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5504] [GtoPdb: 243] [UniProtKB: Q62805] | ||||||||
| ChEMBL | Inhibition of [3H]glycine uptake at rat glycine transporter 1 expressed in african green monkey COS7 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6321-6323 [PMID:19013063] |
| GlyT1/Glycine transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2337] [GtoPdb: 935] [UniProtKB: P48067] | ||||||||
| ChEMBL | Inhibition of uptake of [3H]-glycine into cells transfected with human GlyT-1b transporter | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4027-4030 [PMID:15225720] |
| ChEMBL | Inhibition of human GlyT1 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake incubated for 10 mins at pH 7.4 by scintillation spectroscopy | B | 7.85 | pIC50 | 14.16 | nM | IC50 | ACS Med Chem Lett (2019) 10: 904-910 [PMID:31223446] |
| ChEMBL | Inhibition of human GlyT-1 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2018) 61: 2652-2679 [PMID:28876062] |
| ChEMBL | Inhibition of human GlyT1 expressed in QT6 cells assessed as reduction in [14C]glycine uptake incubated for 20 mins by liquid scintillation counting method | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2020) 63: 3834-3867 [PMID:31774679] |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | Neuropharmacology (2008) 55: 743-54 [PMID:18602930] |
| ChEMBL | Inhibition of GlyT1 in human JAR cells assessed as inhibition of [3H]glycine uptake preincubated for 1 mins measured after 2 hrs by liquid scintillation counting | B | 9.41 | pIC50 | 0.39 | nM | IC50 | Bioorg Med Chem (2011) 19: 6245-6253 [PMID:21975065] |
| GlyT1/Glycine transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4556] [GtoPdb: 935] [UniProtKB: P28572] | ||||||||
| ChEMBL | Displacement of [3H]glycine from GlyT1 in rat C6 glioma cells incubated for 30 mins prior to substrate addition measured after 10 mins by scintillation counting analysis | B | 8.05 | pIC50 | 8.9 | nM | IC50 | J Med Chem (2013) 56: 5744-5756 [PMID:23837744] |
| GlyT2/Glycine transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3060] [GtoPdb: 936] [UniProtKB: Q9Y345] | ||||||||
| ChEMBL | Inhibition of [14C]glycine reuptake at human GlyT2 expressed in BE(2)-C cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5233-5238 [PMID:17629697] |
| ChEMBL | Inhibition of human GlyT2 expressed in porcine aorta epithelial cells assessed as reduction in [3H]-Glycine uptake at pH 7.5 by scintillation spectroscopy | B | 5.74 | pIC50 | 1800 | nM | IC50 | ACS Med Chem Lett (2019) 10: 904-910 [PMID:31223446] |
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]
