MRS 2219 [Ligand Id: 6496] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL74121 (MRS-2220)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2X1/P2X purinoceptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2530] [GtoPdb: 478] [UniProtKB: P47824]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 1 (P2X1) F 4.99 pEC50 10200 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
ChEMBL Inhibition of inward ion current elicited by ATP at P2X1 receptor expressed in Xenopus oocytes F 5.23 pEC50 5900 nM EC50 J Med Chem (2001) 44: 340-349 [PMID:11462975]
ChEMBL Compound was tested in a functional ion channel assay of ATP-induced current at recombinant rat P2X1 receptor expressed in Xenopus oocytes. B 5.23 pEC50 5900 nM EC50 J Med Chem (1998) 41: 2201-2206 [PMID:9632352]
P2X2/P2X purinoceptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2135] [GtoPdb: 479] [UniProtKB: P49653]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 2 (P2X2) at 30 uM F 4 pEC50 100000 nM EC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 3 (P2X2) 10 uM, expressed in Xenopus oocytes F 4.23 pIC50 58300 nM IC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]
P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
ChEMBL The compound was evaluated for antagonist activity against recombinant rat P2X purinoceptor 4 (P2X4) 3 uM F 4 pIC50 >100000 nM IC50 J Med Chem (2002) 45: 4057-4093 [PMID:12213051]

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]