MRS2500 [Ligand Id: 1724] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL444278 (MRS-2500) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | - | - | - |
Biochem Pharmacol (2004) 68: 1995-2002 [PMID:15476670]; J Med Chem (2003) 46: 4974-87 [PMID:14584948] |
| ChEMBL | Inhibition of [3H]5 binding to P2Y purinoceptor 1 expressed in Sf9 cells | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (2003) 46: 4974-4987 [PMID:14584948] |
| ChEMBL | Binding affinity to human P2Y1 receptor | B | 9.11 | pKi | 0.78 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3338-3343 [PMID:18445527] |
| ChEMBL | Displacement of [3H]2-chloro-N 6- methyl-( N )-methanocarba-2'-deoxyadenosine 3 ' ,5 '-bis-phosphate from human P2Y1 expressed in baculovirus infected insect Sf9 cells after 30 mins by scintillation spectrometric method | B | 9.11 | pKi | 0.78 | nM | Ki | Eur J Med Chem (2018) 158: 302-310 [PMID:30223118] |
| ChEMBL | Antagonistic activity against P2Y purinoceptor 1 | F | 8.08 | pIC50 | 8.4 | nM | IC50 | J Med Chem (2003) 46: 4974-4987 [PMID:14584948] |
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]
