(R)-NFPS [Ligand Id: 4618] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL180966 (ALX-5407)
  • GAL1 receptor/Galanin receptor 1 in Rat [ChEMBL: CHEMBL5504] [GtoPdb: 243] [UniProtKB: Q62805]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 32:

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]