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 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]