CGS 24012 [Ligand Id: 418] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2094089
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 6.73 pKi 188 nM Ki J. Med. Chem. (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 6.85 pKi 142 nM Ki J. Med. Chem. (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. B 6.85 pKi 142 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 6.85 pKi 142 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 6.93 pKi 118 nM Ki J. Med. Chem. (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Inhibition of [3H]CHA binding to adenosine A1 receptor from rat brain membranes B 6.97 pKi 108 nM Ki J. Med. Chem. (1992) 35: 2253-2260 [PMID:1613750]
ChEMBL Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 6.99 pKi 103 nM Ki J. Med. Chem. (1992) 35: 241-252 [PMID:1732541]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. B 7.19 pKi 64 nM Ki J. Med. Chem. (1992) 35: 2881-2890 [PMID:1495019]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation F 5.25 pEC50 5623.41 nM EC50 J. Med. Chem. (1991) 34: 1334-1339 [PMID:2016707]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 6.4 pKi - - - J Biol Chem (1995) 270: 13987-97 [PMID:7775460]
ChEMBL Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 7.42 pKi 38.1 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 7.44 pKi 35.9 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 7.72 pKi 18.9 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]

ChEMBL data shown on this page come from version 28:

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]