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 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]
