CV-1808 [Ligand Id: 420] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1256672 (CV-1808)
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  • A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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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 against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 6.11 pKi 780 nM Ki J Med Chem (1992) 35: 241-252 [PMID:1732541]
ChEMBL Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine B 6.16 pKi 689 nM Ki J Med Chem (1990) 33: 1919-1924 [PMID:2362269]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 6.22 pKi 600 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 6.22 pKi 600 nM Ki J Med Chem (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine B 6.23 pKi 590 nM Ki J Med Chem (1988) 31: 271-273 [PMID:3336027]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 6.25 pKi 560 nM Ki J Med Chem (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. B 6.28 pKi 529 nM Ki J Med Chem (1992) 35: 2881-2890 [PMID:1495019]
ChEMBL Binding affinity to rat recombinant adenosine A1 receptor B 6.4 pKi 400 nM Ki J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor B 5.86 pIC50 1380 nM IC50 J Med Chem (1991) 34: 2570-2579 [PMID:1875349]
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 4.9 pEC50 12589.25 nM EC50 J Med Chem (1991) 34: 1334-1339 [PMID:2016707]
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 7.1 pKi - - - Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286];
Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity to rat recombinant adenosine receptor A2a B 7 pKi 100 nM Ki J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 32:

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]