2'-Me-CCPA [Ligand Id: 5591] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL251997
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]