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: CHEMBL317052 (Lexiscan, Regadenoson anhydrous) |
---|
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/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Displacement of [3H]CPX from human adenosine receptor A1 expressed in CHO-K1 cell membranes incubated for 2 hrs by radioligand competitive binding analysis | B | 4.78 | pKi | >16460 | nM | Ki | Eur J Med Chem (2019) 179: 310-324 [PMID:31255928] |
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Binding affinity to human recombinant adenosine A1 receptor | B | 5.42 | pKi | 3770 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]ZM241385 from human adenosine receptor A2A expressed in HEK-293 cell membrane incubated for 2 hrs by radioligand competitive binding analysis | B | 5.9 | pKi | 1269 | nM | Ki | Eur J Med Chem (2019) 179: 310-324 [PMID:31255928] |
ChEMBL | Receptor binding affinity for the adenosine A2A receptor were determined using [3H]ZM-241385 as a radioligand in pig | B | 5.95 | pKi | 1120 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2935-2939 [PMID:12270178] |
ChEMBL | Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells | B | 6.53 | pKi | 297 | nM | Ki | J Med Chem (2004) 47: 4766-4773 [PMID:15341491] |
ChEMBL | Binding affinity to A2A adenosine receptor | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
ChEMBL | Binding affinity to human recombinant adenosine receptor A2a | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Binding affinity to human adenosine A2A receptor | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
GtoPdb | - | - | 6.54 | pKi | 290 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Receptor binding affinity for the adenosine A2A receptor was determined using [3H]ZM-241385 as a radioligand in rat | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2935-2939 [PMID:12270178] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Agonist activity at human recombinant adenosine receptor A2b by cAMP assay | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Binding affinity for Adenosine A3A receptor | B | 5 | pKi | >>10000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2935-2939 [PMID:12270178] |
ChEMBL | Binding affinity to human recombinant adenosine A3 receptor | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells | B | 8 | pKi | >10 | nM | Ki | J Med Chem (2004) 47: 4766-4773 [PMID:15341491] |
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]