ALX 1393 [Ligand Id: 4622] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL475562 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GAL2 receptor/Galanin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5577] [GtoPdb: 244] [UniProtKB: O08726] | ||||||||
| ChEMBL | Inhibition of [3H]glycine uptake at rat glycine transporter 2 expressed in african green monkey COS7 cells | B | 7.68 | pIC50 | 21.1 | 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 human GlyT-1 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake preincubated for 30 mins followed by 3H]-glycine addition measured after 30 mins by liquid scintillation counting method | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2018) 61: 2652-2679 [PMID:28876062] |
| GlyT2/Glycine transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3060] [GtoPdb: 936] [UniProtKB: Q9Y345] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | Br J Pharmacol (2013) 170: 1053-63 [PMID:23962079] |
| ChEMBL | Inhibition of human GlyT-2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake preincubated for 30 mins followed by 3H]-glycine addition measured after 30 mins by liquid scintillation counting method | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2018) 61: 2652-2679 [PMID:28876062] |
| ChEMBL | Inhibition of full length human GlyT2 expressed in FreeStyle 293-F suspension cells incubated for 30 mins before [3H]glycine addition and measured after 30 mins by liquid scintillation counting method | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2019) 62: 2466-2484 [PMID:30714733] |
| 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 | 7.59 | pIC50 | 26 | 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]
