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]
1 CHEMBL219160_lig_chart_1 Adenosine A1 receptor Human
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
2 CHEMBL219160_lig_chart_2 Adenosine A2a receptor Human
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
3 CHEMBL219160_lig_chart_3 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
4 CHEMBL219160_lig_chart_4 Adenosine A3 receptor Human
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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 27:

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]