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 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]