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]
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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]
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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]
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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 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]