BW-A1433 [Ligand Id: 443] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL16997
  • 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]
  • 7.82
1 CHEMBL16997_lig_chart_1 Adenosine A1 receptor HumanRat
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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]
  • 6.1
2 CHEMBL16997_lig_chart_2 Adenosine A2a receptor HumanRat
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • 7.22
3 CHEMBL16997_lig_chart_3 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
  • 4.82
4 CHEMBL16997_lig_chart_4 Adenosine A3 receptor HumanRat
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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 Antagonist activity against recombinant human adenosine A1 receptor expressed in HEK293 cells in presence of [125I]IABA radioligand. F 6.85 pKi 140 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Antagonist activity against adenosine A1 receptor in rat brain membrane in presence of [3H]R-PIA radioligand. F 7.82 pKi 15 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane B 7.82 pKi 15 nM Ki J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL Inhibition of [3H]CCPA binding to rat adenosine A1 receptor B 7.82 pKi 15 nM Ki J. Med. Chem. (2002) 45: 1500-1510 [PMID:11906291]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Antagonist activity against recombinant human adenosine A2A receptor expressed in HEK293 cells in presence of [125I]iodo-ZM-241385 radioligand. F 6.72 pKi 190 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Antagonist activity against adenosine A2A receptor in rat striatal membrane in presence of [3H]CGS-21680 radioligand. F 6.1 pKi 800 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane B 6.1 pKi 800 nM Ki J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor B 6.1 pKi 800 nM Ki J. Med. Chem. (2002) 45: 1500-1510 [PMID:11906291]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX F 7.22 pKi 60 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor B 7.22 pKi 60 nM Ki J. Med. Chem. (2002) 45: 1500-1510 [PMID:11906291]
GtoPdb - - 7.3 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 7.3 pKi - - - Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299]
ChEMBL Antagonist activity against human adenosine A3 receptor expressed in HEK cells in presence of [125]IAB-MECA or [125I]IABA radioligand. F 7.52 pKi 30 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor B 7.52 pKi 30 nM Ki J. Med. Chem. (2002) 45: 1500-1510 [PMID:11906291]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Antagonist activity against rat adenosine A3 receptor using [125I]I-AB-MECA or [125 I]IABA F 4.82 pKi 15000 nM Ki J. Med. Chem. (2000) 43: 1165-1172 [PMID:10737749]
ChEMBL Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA B 4.82 pKi 15000 nM Ki J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565]
GtoPdb - - 7.4 pKi - - - J Biol Chem (1994) 269: 24692-8 [PMID:7929142]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]