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 35:
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]
