2-chloroadenosine [Ligand Id: 372] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285819 (2-Chloroadenosine)
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
  • Adenosine A2a receptor in Guinea pig [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
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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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  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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]
GtoPdb - - 5.6 pKi - - - J. Biol. Chem. (1994) 269: 32077-84 [PMID:7798201];
J. Biol. Chem. (1999) 274: 3617-21 [PMID:9920910]
ChEMBL Displacement of [3H]CPX from adenosine A1 receptor B 7.74 pKi 18.4 nM Ki J. Nat. Prod. (1993) 56: 441-455 [PMID:8496700]
ChEMBL Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method B 8.55 pKi 2.8 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Binding affinity to human recombinant adenosine A1 receptor B 8.86 pKi 1.39 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain B 7.6 pKi 25 nM Ki J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 7.69 pKi 20.2 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1988) 31: 271-273 [PMID:3336027]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. B 8.03 pKi 9.3 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 8.06 pKi 8.74 nM Ki J. Med. Chem. (1985) 28: 1383-1384 [PMID:2995663]
GtoPdb - - 8.17 pKi 6.7 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Binding affinity towards adenosine A1 receptor in rat brain cortex B 8.17 pKi 6.7 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Binding affinity towards adenosine A1 receptor in rat brain cortex B 8.17 pKi 6.7 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor B 8.17 pKi 6.7 nM Ki J. Med. Chem. (1991) 34: 3388-3390 [PMID:1766003]
ChEMBL Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor B 7.43 pIC50 37 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 6.72 pEC50 190.55 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]
ChEMBL Binding affinity to human recombinant adenosine receptor A2a B 6.74 pKi 180 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb - - 6.8 pKi - - - J. Biol. Chem. (1995) 270: 13987-97 [PMID:7775460];
Biochem. Pharmacol. (1999) 57: 65-75 [PMID:9920286]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 6.92 pKi 120 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity towards adenosine A2A receptor in rat brain striatum B 7.12 pKi 76 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Binding affinity towards adenosine A2A receptor in rat brain striatum B 7.12 pKi 76 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Inhibition of [3H]- NECA binding to adenosine receptor A2A B 7.12 pKi 76 nM Ki J. Med. Chem. (1991) 34: 3388-3390 [PMID:1766003]
GtoPdb - - 7.12 pKi 76 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 7.2 pKi 63 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand B 7.2 pKi 63 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain B 8.1 pKi 8 nM Ki J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
ChEMBL Antagonism of cyclic [3H]AMP accumulation elicited by 15 uM 2-chloroadenosine in [3H]adenine-labeled guinea pig cerebral cortical slices at A2 receptor F 5.1 pEC50 8000 nM EC50 J. Med. Chem. (1985) 28: 487-492 [PMID:2984420]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells B 4.59 pKi 25500 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells B 4.67 pKi 21400 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb - - 5 pKi - - - Mol. Pharmacol. (1999) 56: 705-13 [PMID:10496952];
Mol. Pharmacol. (2000) 58: 1349-56 [PMID:11093773];
Can. J. Physiol. Pharmacol. (1980) 58: 673-91 [PMID:6253037]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase F 3.72 pEC50 -3.72 - logEC50 J. Med. Chem. (2008) 51: 2088-2099 [PMID:18321038]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells B 4.94 pKi 11600 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells B 6.19 pKi 650 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 7.06 pKi 87 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity to human recombinant adenosine A3 receptor B 7.72 pKi 19 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 5.79 pEC50 1630 nM EC50 J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 5.49 pKi 3200 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
GtoPdb - - 5.72 pKi 1890 nM Ki Mol. Pharmacol. (1994) 45: 1101-11 [PMID:8022403]
ChEMBL Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA B 5.72 pKi 1890 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor B 5.72 pKi 1890 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
Adenosine deaminase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2966] [UniProtKB: P56658]
ChEMBL Inhibition of calf placental adenosine deaminase by Lineweaver-Burk plot analysis B 4.26 pKi 54500 nM Ki J. Med. Chem. (2011) 54: 107-121 [PMID:21138280]
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of recombinant human PDE2A catalytic domain (580 to 919 residues) expressed in Escherichia coli BL21 (Codonplus) using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2018) 26: 119-133 [PMID:29174506]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 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 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 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 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 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 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]

ChEMBL data shown on this page come from version 26:

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]