VUF5574 [Ligand Id: 3280] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL70880 (VUF-5574)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • 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]
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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]
GtoPdb - - 5 pKi <10000 nM Ki J Med Chem (1998) 41: 3987-93 [PMID:9767636]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptor of rat brain cortical membrane B 5 pKi >10000 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 5 pKi <10000 nM Ki J Med Chem (1998) 41: 3987-93 [PMID:9767636]
ChEMBL Displacement of [3H]-CGS- 21680 binding in adenosine A2A receptor of rat striatal membrane B 5 pKi >10000 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Percent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cells B 5 pKi 10000 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity by its ability to displace [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 5.39 pKi 4030 nM Ki J Med Chem (2000) 43: 2227-2238 [PMID:10841801]
GtoPdb - - 8.39 pKi 4.03 nM Ki J Med Chem (2000) 43: 2227-38 [PMID:10841801]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in HEK 293 cells B 8.4 pKi 4 nM Ki J Med Chem (2001) 44: 749-762 [PMID:11262085]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.6 pIC50 2511.89 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]

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]