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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]