2-chloroadenosine [Ligand Id: 372] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL285819 (2-Chloroadenosine) |
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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] |
| heat shock protein 90 beta family member 1/Endoplasmin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625] | ||||||||
| ChEMBL | Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay | B | 5.07 | pKd | 8600 | nM | Kd | ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064] |
| ChEMBL | Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay | B | 5.74 | pKi | 1800 | nM | Ki | ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064] |
| 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 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]
