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ChEMBL ligand: CHEMBL251997 |
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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 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane | B | 4.92 | pKi | 12000 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 8.47 | pKi | 3.37 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Binding affinity for human adenosine A1 receptor subtype expressed in CHO cells | B | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane | B | 5.34 | pKi | 4560 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
ChEMBL | Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Binding affinity to bovine adenosine A1 receptor assessed as inhibition constant | B | 8.74 | pKi | 1.8 | nM | Ki | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Binding affinity for human adenosine A2a receptor subtype expressed in CHO cells | B | 5.02 | pKi | 9580 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 5.02 | pKi | 9580 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes | B | 5.34 | pKi | 4560 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
ChEMBL | Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Binding affinity for human adenosine A2b receptor subtype expressed in CHO cells | B | 4.42 | pKi | 37600 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
ChEMBL | Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity | F | 5.94 | pKi | 1150 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells | B | 4.42 | pKi | 37600 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes | B | 5.07 | pKi | 8570 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
ChEMBL | Binding affinity for human adenosine A3 receptor subtype expressed in CHO cells | B | 5.94 | pKi | 1150 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
GtoPdb | - | - | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (1998) 41: 1708-15 [PMID:9572897] |
ChEMBL | Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes | B | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL | Binding affinity to rat adenosine A3 receptor assessed as inhibition constant | B | 5.3 | pKi | 5000 | nM | Ki | RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182] |
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]