CVT-6883 [Ligand Id: 5615] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL260933 (CVT-6883, GS-6201)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
1 CHEMBL260933_lig_chart_1 Adenosine A1 receptor Human
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
2 CHEMBL260933_lig_chart_2 Adenosine A2a receptor Human
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
3 CHEMBL260933_lig_chart_3 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
4 CHEMBL260933_lig_chart_4 Adenosine A3 receptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Binding affinity to human adenosine A1 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.71 pKi 1940 nM Ki J. Med. Chem. (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [3H]CPX from human recombinant adenosine A1 receptor expressed in CHO cells B 5.71 pKi 1940 nM Ki J. Med. Chem. (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A1 receptor B 5.71 pKi 1940 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity to human adenosine A2A receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.48 pKi 3280 nM Ki J. Med. Chem. (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [3H]ZM-241385 from human recombinant adenosine A2A receptor expressed in HEK293 cells B 5.48 pKi 3280 nM Ki J. Med. Chem. (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A2A receptor B 5.48 pKi 3280 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 7.66 pKi 22 nM Ki J. Med. Chem. (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A2B receptor B 7.66 pKi 22 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 7.66 pKi 22 nM Ki J. Med. Chem. (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells B 8.08 pKi 8.3 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to human adenosine A3 receptor B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 797-811 [PMID:22148859]
GtoPdb - - 5.97 pKi 1070 nM Ki J. Med. Chem. (2008) 51: 2267-78 [PMID:18321039]
ChEMBL Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in CHO cells B 5.97 pKi 1070 nM Ki J. Med. Chem. (2008) 51: 2267-2278 [PMID:18321039]
ChEMBL Binding affinity to human adenosine A3 receptor B 5.97 pKi 1070 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]

ChEMBL data shown on this page come from version 27:

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]