MRS2578 [Ligand Id: 1753] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1321988 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
| ChEMBL | Antagonist activity at human P2Y6R expressed in HEK293 cells assessed as inhibition of UDP-induced IP3 production preincubated for 0.5 hrs followed by UDP stimulation by ELISA | F | 4.4 | pIC50 | 39450 | nM | IC50 | J Med Chem (2022) 65: 15967-15990 [PMID:36394994] |
| GtoPdb | - | - | 7.4 | pIC50 | - | - | - | Biochem Pharmacol (2004) 67: 1763-70 [PMID:15081875] |
| ChEMBL | Antagonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced inositol-1-phosphate accumulation preincubated for 30 mins followed by UDP addition and measured after 30 mins by liquid scintillation counting method | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2021) 41: 128008-128008 [PMID:33831560] |
| ChEMBL | Antagonist activity at P2Y6 receptor (unknown origin) | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2018) 26: 366-375 [PMID:29254895] |
| ChEMBL | Antagonist activity at human P2Y6 | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2016) 59: 9981-10005 [PMID:27413802] |
| ChEMBL | Antagonist activity at human P2Y6R expressed in human 1321N1 cells assessed as inhibition of UDP-induced calcium mobilization | F | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2023) 66: 6315-6332 [PMID:37078976] |
| ChEMBL | Antagonist activity at human P2Y6R expressed in human 1321N1 cells assessed as inhibition of UDP-induced calcium mobilization incubated for 5 mins followed by agonist stimulation by FLIPR assay | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2022) 75: 128981-128981 [PMID:36089113] |
| ChEMBL | Antagonist activity at human P2Y6R expressed in HEK293 cells assessed as inhibition of UDP-induced IP3 production preincubated for 0.5 hrs followed by UDP stimulation and measured after 12 hrs by ELISA analysis | F | 7.56 | pIC50 | 27.47 | nM | IC50 | J Med Chem (2023) 66: 6315-6332 [PMID:37078976] |
| P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3543] [GtoPdb: 326] [UniProtKB: Q63371] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | - | - | - | Biochem Pharmacol (2004) 67: 1763-70 [PMID:15081875] |
| ChEMBL | Antagonist activity at rat P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced inositol-1-phosphate accumulation preincubated for 30 mins followed by UDP addition and measured after 30 mins by liquid scintillation counting method | F | 7.01 | pIC50 | 98 | nM | IC50 | Bioorg Med Chem Lett (2021) 41: 128008-128008 [PMID:33831560] |
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]
