tecadenoson [Ligand Id: 5592] activity data from GtoPdb and ChEMBL
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: CHEMBL392149 (CVT-510, Tecadenoson) |
|---|
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!
|
|
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 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11] | ||||||||
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane | B | 5.01 | pKi | 9756 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane | B | 8.12 | pKi | 7.6 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Agonist activity at adenosine A1 receptor in pig cortical membrane assessed as stimulation of GTPgammaS binding | F | 7.5 | pEC50 | 31.6 | nM | EC50 | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Displacement of [3H]CPX from adenosine A1 receptor expressed in DDT1 MF2 cells | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| ChEMBL | Binding affinity for adenosine A1 receptor determined using hamster DDT1 cell membranes with [3H]CCPA as radioligand | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 535-539 [PMID:14698198] |
| ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 8.69 | pKi | 2.05 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Agonist activity at adenosine A1 receptor expressed in DDT1 MF2 cells assessed as inhibition of (-)-isoproterenol-stimulated cAMP accumulation | F | 8.09 | pIC50 | 8.2 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| A1 receptor in Pig [GtoPdb: 18] | ||||||||
| GtoPdb | - | - | 8.19 | pKi | 6.5 | nM | Ki |
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]; Biochim Biophys Acta (2011) 1808: 1290-308 [PMID:21185259] |
| Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane | B | 5.14 | pKi | 7300 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
| ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CPX in guinea pig DDT membrane; 543+/-182 | B | 6.27 | pKi | 543 | nM | Ki low | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CCPA in guinea pig DDT membrane; 3.25+/-0.74 | B | 8.49 | pKi | 3.25 | nM | Ki high | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| ChEMBL | Agonistic activity against adenosine A1 receptor in guinea pig isolated hearts | F | 7.39 | pEC50 | 41 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 5.19 | pKi | 6390 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A2A receptor in Pig [GtoPdb: 19] | ||||||||
| GtoPdb | - | - | 5.64 | pKi | 2315 | nM | Ki |
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]; Biochim Biophys Acta (2011) 1808: 1290-308 [PMID:21185259] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity | F | 6.64 | pKi | 227 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells | B | 4.59 | pKi | 25800 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
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]
