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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 |
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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 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]