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ChEMBL ligand: CHEMBL8565 (PSB-1115) |
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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 | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 1500-10 [PMID:11906291] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2006) 49: 4384-4391 [PMID:16821798] |
ChEMBL | Displacement of [3H]CCPA from recombinant human A1 adenosine receptor expressed in CHO cell membranes measured after 20 hrs by microplate filtration based radioligand binding assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612] | ||||||||
ChEMBL | Displacement of [3H]DPCPX from recombinant mouse A1 adenosine receptor expressed in CHO cell membranes measured after 60 mins by liquid scintillation counting method | B | 6.23 | pKi | 591 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (1993) 36: 3341-3349 [PMID:8230124] |
ChEMBL | Displacement of [3H]R-PIA from adenosine A1 receptor in rat brain cortical membranes | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2006) 49: 4384-4391 [PMID:16821798] |
ChEMBL | Displacement of [3H]CCPA from A1 adenosine receptor in rat cortex membranes measured after 60 mins by liquid scintillation counting method | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
GtoPdb | - | - | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (1993) 36: 3341-9 [PMID:8230124] |
ChEMBL | Displacement of [3H]-CCPA from adenosine A1 receptor of rat brain cortical membrane preparations | B | 5.91 | pKi | 1238 | nM | Ki | J Med Chem (2004) 47: 1031-1043 [PMID:14761205] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]MSX-2 from recombinant human A2A adenosine receptor expressed in CHO cell membranes measured after 60 mins by liquid scintillation counting method | B | 5.42 | pKi | 3790 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613] | ||||||||
ChEMBL | Displacement of [3H]MSX-2 from recombinant mouse A2A adenosine receptor expressed in CHO cell membranes measured after 60 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]R-PIA from adenosine A2A receptor in rat brain striatal membranes | B | 4.62 | pKi | 24000 | nM | Ki | J Med Chem (2006) 49: 4384-4391 [PMID:16821798] |
ChEMBL | Displacement of [3H]NECA from rat A2A adenosine receptor expressed in CHO cell membranes measured after 60 mins by liquid scintillation counting method | B | 4.62 | pKi | 24000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
GtoPdb | - | - | 4.62 | pKi | 24000 | nM | Ki | J Med Chem (1993) 36: 3341-9 [PMID:8230124] |
ChEMBL | Displacement of [3H]MSX-2 from adenosine A2A receptor of rat brain striatal membranes | B | 4.93 | pKi | 11800 | nM | Ki | J Med Chem (2004) 47: 1031-1043 [PMID:14761205] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay | B | 6.71 | pKi | 194.98 | nM | Ki | RSC Med Chem (2022) 13: 850-856 [PMID:35923720] |
ChEMBL | Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay | B | 6.72 | pKi | 190.55 | nM | Ki | RSC Med Chem (2022) 13: 850-856 [PMID:35923720] |
GtoPdb | - | - | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2002) 45: 1500-10 [PMID:11906291] |
ChEMBL | Displacement of [3H]ZM241385 from human recombinant adenosine A2B receptor | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2017) 60: 3372-3382 [PMID:28368607] |
ChEMBL | Displacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting method | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
ChEMBL | Antagonist activity at human A2B receptor | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2021) 64: 458-480 [PMID:33372800] |
ChEMBL | Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cells | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2006) 49: 4384-4391 [PMID:16821798] |
ChEMBL | Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2021) 64: 7156-7178 [PMID:34019396] |
ChEMBL | Displacement of [3H]ZM241385 from human recombinant Adenosine A2B receptor | B | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2016) 59: 1967-1983 [PMID:26824742] |
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
ChEMBL | Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method | B | 5.71 | pKi | 1940 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
ChEMBL | Displacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method | B | 5.5 | pKi | 3140 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 1500-10 [PMID:11906291] |
ChEMBL | Displacement of [3H]PSB11 from human recombinant adenosine A3 receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2006) 49: 4384-4391 [PMID:16821798] |
ChEMBL | Displacement of [3H]PSB-11 from recombinant human A3 adenosine receptor expressed in CHO cell membranes by radioligand binding assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
ChEMBL | Displacement of [3H]NECA from recombinant mouse A3 adenosine receptor expressed in CHO cell membranes measured after 180 mins by liquid scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Binding affinity to rat A3 adenosine receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2019) 62: 4032-4055 [PMID:30835463] |
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]