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ChEMBL ligand: CHEMBL17002 |
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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 against recombinant human adenosine A1 receptor expressed in HEK293 cells in presence of [125I]IABA radioligand. | F | 6.8 | pKi | 157 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Antagonist activity against human adenosine A1 receptor | F | 6.8 | pKi | 157 | nM | Ki | Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. | F | 7.42 | pKi | 37.6 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. | F | 6.95 | pKi | 112 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Antagonist activity against human adenosine A2A receptor | F | 6.95 | pKi | 112 | nM | Ki | Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. | F | 6.26 | pKi | 548 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX | F | 8.86 | pKi | 1.39 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Antagonist activity against human adenosine A2B receptor | F | 8.86 | pKi | 1.39 | nM | Ki | Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. | F | 6.64 | pKi | 230 | nM | Ki | J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Antagonist activity against human adenosine A3 receptor | F | 6.64 | pKi | 230 | nM | Ki | Eur. J. Med. Chem. (2010) 45: 3459-3471 [PMID:20537438] |
ChEMBL data shown on this page come from version 31:
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]