Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL410873 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
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 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]