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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 |
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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 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]