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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] |
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 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]