LAS38096 [Ligand Id: 5617] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL375293 (LAS38096)
  • 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]
  • A2B receptor/Adenosine A2b receptor in Mouse [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
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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 after 90 mins by filtration binding assay B 5.55 pKi 2821 nM Ki Bioorg Med Chem Lett (2010) 20: 1697-1700 [PMID:20137946]
GtoPdb - - 5.55 pKi 2821 nM Ki J Med Chem (2007) 50: 2732-6 [PMID:17469811];
Bioorg Med Chem Lett (2010) 20: 1697-700 [PMID:20137946]
ChEMBL Displacement of [3H]DPCPX from human A1 receptor expressed in CHO cells B 6 pKi >1000 nM Ki J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]ZM-241385 from human A2A receptor expressed in HeLa cells B 5.6 pKi >2500 nM Ki J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
GtoPdb - - 6 pKi >1000 nM Ki J Med Chem (2007) 50: 2732-6 [PMID:17469811];
Bioorg Med Chem Lett (2010) 20: 1697-700 [PMID:20137946]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells B 7.77 pKi 17 nM Ki J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
ChEMBL Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay B 7.77 pKi 17 nM Ki Bioorg Med Chem Lett (2010) 20: 1697-1700 [PMID:20137946]
GtoPdb - - 7.77 pKi 17 nM Ki J Med Chem (2007) 50: 2732-6 [PMID:17469811];
Bioorg Med Chem Lett (2010) 20: 1697-700 [PMID:20137946]
ChEMBL Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA F 6.49 pIC50 321 nM IC50 J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
ChEMBL Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA F 6.19 pIC50 640 nM IC50 J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
ChEMBL Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA F 6.46 pIC50 349 nM IC50 J Med Chem (2007) 50: 2732-2736 [PMID:17469811]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5.98 pKi 1043 nM Ki J Med Chem (2007) 50: 2732-6 [PMID:17469811];
Bioorg Med Chem Lett (2010) 20: 1697-700 [PMID:20137946]
ChEMBL Displacement of [3H]NECA from human adenosine A3 receptor expressed in human HeLa cells after 3 hrs by filtration binding assay B 5.98 pKi 1043 nM Ki Bioorg Med Chem Lett (2010) 20: 1697-1700 [PMID:20137946]
ChEMBL Displacement of [2H]NECA from human A3 receptor expressed in HeLa cells B 6 pKi >1000 nM Ki J Med Chem (2007) 50: 2732-2736 [PMID:17469811]

ChEMBL data shown on this page come from version 32:

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]