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 33:
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]
