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 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]
