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ChEMBL ligand: CHEMBL223270 |
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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/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - | J Med Chem (2002) 45: 3271-9 [PMID:12109910] |
ChEMBL | Binding affinity against Human recombinant Adenosine A1 receptor stably transfected in CHO cells using [3H]CCPA as radioligand | B | 6.25 | pKi | 560 | nM | Ki | J Med Chem (2002) 45: 3271-3279 [PMID:12109910] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 6.25 | pKi | 560 | nM | Ki | J Med Chem (2007) 50: 1222-1230 [PMID:17309246] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity towards adenosine A1 receptor in rat brain cortex | B | 6.16 | pKi | 698 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 6.16 | pKi | 698 | 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 | 6.16 | pKi | 698 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
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 | 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/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
GtoPdb | - | - | 6.2 | pKi | - | - | - | J Med Chem (2002) 45: 3271-9 [PMID:12109910] |
ChEMBL | Binding affinity against Human recombinant Adenosine A2A receptor stably transfected in CHO cells using [3H]NECA as radioligand | B | 6.21 | pKi | 620 | nM | Ki | J Med Chem (2002) 45: 3271-3279 [PMID:12109910] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 6.21 | pKi | 620 | nM | Ki | J Med Chem (2007) 50: 1222-1230 [PMID:17309246] |
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 | 6.92 | pKi | 120 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
ChEMBL | Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. | B | 6.92 | pKi | 120 | 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 | 6.92 | pKi | 120 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Functional activity against adenosine A2a receptor from rat aorta. | F | 5.82 | pEC50 | 1500 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Vasorelaxation as Adenosine A2A receptor activity in rat aorta | F | 9 | pEC50 | >1 | nM | EC50 | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand | B | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2002) 45: 3271-3279 [PMID:12109910] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 8.2 | pKi | - | - | - | J Med Chem (2002) 45: 3271-9 [PMID:12109910] |
ChEMBL | Binding affinity against Human recombinant Adenosine A3 receptor stably transfected in CHO cells using [3H]NECA as radioligand | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2002) 45: 3271-3279 [PMID:12109910] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2007) 50: 1222-1230 [PMID:17309246] |
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]