LUF5981 [Ligand Id: 5607] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL219160 (LUF-5981)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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]
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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]DPCPX from human adenosine A1 receptor expressed in CHO cells B 9.05 pKi 0.9 nM Ki J Med Chem (2007) 50: 828-834 [PMID:17300165]
GtoPdb - - 9.05 pKi 0.9 nM Ki J Med Chem (2007) 50: 828-34 [PMID:17300165]
ChEMBL Activity at human adenosine A1 receptor in CHO cells assessed as effect on CPA induced inhibition of forskolin-stimulated cAMP production F 5.77 pIC50 1700 nM IC50 J Med Chem (2007) 50: 828-834 [PMID:17300165]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 6.71 pKi 194 nM Ki J Med Chem (2007) 50: 828-34 [PMID:17300165]
ChEMBL Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in CHO cells B 6.71 pKi 194 nM Ki J Med Chem (2007) 50: 828-834 [PMID:17300165]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 6.52 pKi >300 nM Ki Neurology (2003) 61: S97-100 [PMID:14663020]
ChEMBL Displacement of [3H]MRS1754 from human adenosine A2B receptor B 6.52 pKi 300 nM Ki J Med Chem (2007) 50: 828-834 [PMID:17300165]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 6.2 pKi 637 nM Ki J Med Chem (2007) 50: 828-834 [PMID:17300165]
GtoPdb - - 6.2 pKi 637 nM Ki J Med Chem (2007) 50: 828-34 [PMID:17300165]

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]