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ChEMBL ligand: CHEMBL410873 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
GtoPdb | - | - | 7.2 | pKi | - | - | - | J Med Chem (2002) 45: 3271-9 [PMID:12109910] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX | B | 5.5 | pKi | 3160 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. | B | 6.56 | pKi | 276 | nM | Ki | J Med Chem (1992) 35: 2881-2890 [PMID:1495019] |
ChEMBL | Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX | B | 6.87 | pKi | 136 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
ChEMBL | Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
ChEMBL | Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA | B | 7.36 | pKi | 43.9 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Inhibition of adenylate cyclase via adenosine A1 receptors in rat fat cell membranes | F | 5.36 | pIC50 | 4380 | nM | IC50 | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Functional activity against adenosine A1 receptor from rat atria. | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
ChEMBL | Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria | F | 9 | pEC50 | >1 | nM | EC50 | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
GtoPdb | - | - | 8.3 | pKi | - | - | - |
J Med Chem (2002) 45: 3271-9 [PMID:12109910]; 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 | Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
ChEMBL | Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
ChEMBL | Vasorelaxation as Adenosine A2A receptor activity in rat aorta | F | 6.22 | pEC50 | 596 | nM | EC50 | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
ChEMBL | Functional activity against adenosine A2a receptor from rat aorta. | F | 6.22 | pEC50 | 596 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
A3 receptor in Human [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 8.6 | pKi | - | - | - | J Med Chem (2002) 45: 3271-9 [PMID:12109910] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
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 | 7.59 | pKi | 25.6 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
GtoPdb | - | - | 6.6 | pKi | - | - | - | Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300] |
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]