PSB-10 [Ligand Id: 5619] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1562432
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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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]
ChEMBL Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay B 5.77 pKi 1700 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
GtoPdb - - 5.77 pKi 1700 nM Ki Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
GtoPdb - - 6.09 pKi 805 nM Ki J Med Chem (2002) 45: 3440-50 [PMID:12139454]
ChEMBL Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay B 6.09 pKi 805 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay B 5.57 pKi 2700 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
GtoPdb - - 5.57 pKi 2700 nM Ki Bioorg Med Chem (2003) 11: 347-56 [PMID:12517430]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]MSX2 from adenosine receptor A2A in rat brain striatum membranes incubated for 30 mins by radioligand competition assay B 5.22 pKi 6040 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
GtoPdb - - 5.22 pKi 6040 nM Ki J Med Chem (2002) 45: 3440-50 [PMID:12139454]
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 receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay B 4.52 pKi 30000 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 5.68 pKi 2100 nM Ki J Med Chem (2002) 45: 3440-50 [PMID:12139454]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 B 8.02 pKi 9.54 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 9.36 pKi 0.44 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [3H]PSB-11 from human adenosine receptor A3 expressed in CHO cell membranes incubated for 60 mins by radioligand competition assay B 9.36 pKi 0.44 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
GtoPdb - - 9.36 pKi 0.44 nM Ki J Med Chem (2002) 45: 3440-50 [PMID:12139454]
ChEMBL Inverse agonist activity at human recombinant A3 adenosine receptor expressed CHO cells by [35S]GTPgammaS binding assay F 8.4 pIC50 4 nM IC50 J Med Chem (2011) 54: 5205-5220 [PMID:21675777]

ChEMBL data shown on this page come from version 32:

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]