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ChEMBL ligand: CHEMBL447664 (Biib014, BIIB-014, BIIB014, CEB-4520, V-2006, V2006, VER-11135, VER-A-00049, VER-A00049, VER-A-00-11, VER-A00-11, VER-ADO-49, Vipadenant) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Antagonist activity at human adenosine A1 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay | F | 7 | pKd | 100 | nM | Kd | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Displacement of radioligand from human recombinant adenosine A1 receptor at 21 degC after 90 mins by cell-based microplate scintillation counting | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Inhibition of human recombinant adenosine A1 receptor | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
GtoPdb | - | - | 7.17 | pKi | 68 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay | F | 9.2 | pKd | 0.63 | nM | Kd | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Displacement of radioligand from human recombinant adenosine A2A receptor at 21 degC after 90 mins by cell-based microplate scintillation counting | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Inhibition of human recombinant adenosine receptor A2a | F | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay | F | 7.5 | pKd | 31.62 | nM | Kd | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
GtoPdb | - | - | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Inhibition of human recombinant adenosine receptor A2b | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Antagonist activity at human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay | F | 5.8 | pKd | 1584.89 | nM | Kd | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Displacement of radioligand from human recombinant adenosine A3 receptor at 21 degC after 60 mins by cell-based microplate scintillation counting | B | 6 | pKi | 1005 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
ChEMBL | Inhibition of human recombinant adenosine A3 receptor | B | 6 | pKi | 1005 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
GtoPdb | - | - | 6 | pKi | 1005 | nM | Ki | J Med Chem (2009) 52: 33-47 [PMID:19072055] |
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]