Org 25543 [Ligand Id: 4667] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL88588 (ORG-25543) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GlyT1/Glycine transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2337] [GtoPdb: 935] [UniProtKB: P48067] | ||||||||
| ChEMBL | Inhibition of human GlyT-1 expressed in CHO cells assessed as reduction in [3H]-glycine uptake | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 2652-2679 [PMID:28876062] |
| ChEMBL | In vitro inhibition of human Glycine Transporter type-1. | B | 7 | pIC50 | >100 | nM | IC50 | J Med Chem (2001) 44: 2679-2682 [PMID:11495577] |
| 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 | 7.66 | pIC50 | 22 | 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 human Glycine Transporter type-2 | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2001) 44: 2679-2682 [PMID:11495577] |
| ChEMBL | Inhibition of human GlyT-2 expressed in CHO cells assessed as reduction in [3H]-glycine uptake | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2018) 61: 2652-2679 [PMID:28876062] |
| ChEMBL | Inhibition of human GlyT2 stably expressed in CHO cells assessed as reduction in [3H]glycine uptake incubated for 10 mins by liquid scintillation counting method | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2020) 63: 3834-3867 [PMID:31774679] |
| ChEMBL | Inhibition of recombinant human GlyT2 | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2019) 62: 2466-2484 [PMID:30714733] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2001) 44: 2679-82 [PMID:11495577] |
| ChEMBL | Inhibition of recombinant human GlyT2a expressed in Xenopus laevis oocytes assessed as reduction in channel current by two-electrode voltage clamp electrophysiology | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2019) 62: 2466-2484 [PMID:30714733] |
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]
