PSB1115 [Ligand Id: 3286] 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: CHEMBL8565 (PSB-1115)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Mouse [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Mouse [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
There should be some charts here, you may need to enable JavaScript!
  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor/Adenosine A2b receptor in Mouse [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Mouse [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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]
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]