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ChEMBL ligand: CHEMBL27041 |
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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 | 6.76 | pKi | 175 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
ChEMBL | Binding affinity for adenosine A1 receptor as inhibition of [125-I]-labeled aminobenzyl adenosine binding to bovine brain membranes | B | 7.77 | pKd | 17 | nM | Kd | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity to rat adenosine A1 receptor | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2006) 49: 282-299 [PMID:16392813] |
ChEMBL | Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. | F | 7.24 | pKi | 58 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1989) 32: 1873-1879 [PMID:2754711] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat cerebral cortical membranes by [3H]cyclohexyladenosine displacement. | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1985) 28: 1334-1340 [PMID:2993622] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 7.24 | pKi | 58 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Inhibition of [3H]- PIA binding at adenosine A1 receptor on rat cerebral cortex membranes. | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1987) 30: 211-214 [PMID:3806597] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Binding affinity to recombinant human adenosine A2A receptor | B | 6.07 | pKi | 851.14 | nM | Ki | J Med Chem (2006) 49: 282-299 [PMID:16392813] |
ChEMBL | Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. | F | 6.23 | pKi | 595 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Binding affinity to rat adenosine A2A receptor | B | 5.65 | pKi | 2238.72 | nM | Ki | J Med Chem (2006) 49: 282-299 [PMID:16392813] |
ChEMBL | Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. | F | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - | Biochem Pharmacol (2001) 61: 657-63 [PMID:11266650] |
ChEMBL | Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX | F | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
ChEMBL | Binding affinity to recombinant human adenosine A2B receptor | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2006) 49: 282-299 [PMID:16392813] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Binding affinity to recombinant human adenosine A3 receptor | B | 5.4 | pKi | 3981.07 | nM | Ki | J Med Chem (2006) 49: 282-299 [PMID:16392813] |
ChEMBL | Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. | F | 5.41 | pKi | 3910 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Antagonist activity against rat adenosine A3 receptor using [125I]I-AB-MECA or [125 I]IABA | F | 4.12 | pKi | 75700 | nM | Ki | J Med Chem (2000) 43: 1165-1172 [PMID:10737749] |
ChEMBL | Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA | B | 4.12 | pKi | 75700 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]