PSB1115 [Ligand Id: 3286] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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] | ||||||||
| GtoPdb | - | - | 7.27 | pKi | 53.4 | nM | Ki | J Med Chem (2002) 45: 1500-10 [PMID:11906291] |
| 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 [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] |
| 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] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
