VUF8507 [Ligand Id: 476] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL71053 (VUF-8507)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptor of rat brain cortical membrane B 5.49 pKi 3200 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor of rat brain cortical membrane B 5.49 pKi 3200 nM Ki J Med Chem (2000) 43: 2227-2238 [PMID:10841801]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Tested for antagonist activity by displacement of specific [125I]AB-MECA binding at human Adenosine A3 receptor expressed in HEK 293 cells. B 3.7 pKi 200000 nM Ki J Med Chem (1998) 41: 3994-4000 [PMID:9767637]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 6.7 pKi 200 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
ChEMBL Binding affinity by its ability to displace [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 6.7 pKi 200 nM Ki J Med Chem (2000) 43: 2227-2238 [PMID:10841801]
ChEMBL Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells B 6.7 pKi 200 nM Ki J Med Chem (2006) 49: 4085-4097 [PMID:16821770]
GtoPdb - - 6.7 pKi - - - J Med Chem (1998) 41: 3994-4000 [PMID:9767637]

ChEMBL data shown on this page come from version 33:

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]