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ChEMBL ligand: CHEMBL2333770 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
GtoPdb | Inhibition of [3H]2MeSADP binding to P2Y1 receptors expressed in COS-7 cells. | - | 6.92 | pKi | 120 | nM | Ki | Nature (2015) 520: 317-21 [PMID:25822790] |
ChEMBL | Displacement of [beta-33P]-2MeS-ADP from human P2Y1 receptor transfected in HEK293 cells assessed as residual [beta-33P] bound to plate after 1 hr by scintillation counting analysis | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
ChEMBL | Binding affinity to human P2Y1 receptor | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3239-3243 [PMID:23602442] |
ChEMBL | Displacement of [33P]-2MeS-ADP from human P2Y1 receptor expressed in HEK293 cells after 1 hr by scintillation counting analysis | B | 8.22 | pKi | 6 | nM | Ki | J Med Chem (2013) 56: 9275-9295 [PMID:24164581] |
ChEMBL | Antagonist activity at P2Y1 receptor in platelet-enriched human plasma assessed as 2.5 uM ADP-induced platelet aggregation preincubated for 1 min followed by ADP induction measured at 5 mins by aggregometric analysis | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2013) 56: 9275-9295 [PMID:24164581] |
ChEMBL | Antagonist activity at P2Y1 (unknown origin) expressed in human 1321N1 cells assessed as induction of calcium stimulation by fluo-4 dye based assay | F | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2018) 158: 302-310 [PMID:30223118] |
ChEMBL | Antagonist activity at P2Y1 receptor in washed human platelets assessed as 1 uM 2-methylthio-ADP-induced calcium flux by FLIPR assay | F | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2013) 56: 9275-9295 [PMID:24164581] |
P2Y11 receptor/Purinergic receptor P2Y11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4867] [GtoPdb: 327] [UniProtKB: Q96G91] | ||||||||
ChEMBL | Inhibition of human P2Y11 receptor | B | 4.82 | pKi | >15000 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] | ||||||||
ChEMBL | Displacement of [beta-33P]-2MeS-ADP from human P2Y12 receptor transfected in HEK293 cells assessed as [beta-33P] bound to cells after 1 hr by scintillation counting analysis | B | 4.15 | pKi | >70000 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
P2Y14 receptor/Purinergic receptor P2Y14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4518] [GtoPdb: 330] [UniProtKB: Q15391] | ||||||||
ChEMBL | Inhibition of human P2Y14 receptor | B | 5.46 | pKi | 3500 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
P2Y2 receptor/Purinergic receptor P2Y2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4398] [GtoPdb: 324] [UniProtKB: P41231] | ||||||||
ChEMBL | Inhibition of human P2Y2 receptor | B | 4.82 | pKi | >15000 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
P2Y6 receptor/Pyrimidinergic receptor P2Y6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4714] [GtoPdb: 326] [UniProtKB: Q15077] | ||||||||
ChEMBL | Inhibition of human P2Y6 receptor | B | 4.82 | pKi | >15000 | nM | Ki | J Med Chem (2013) 56: 1704-1714 [PMID:23368907] |
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]