lenrispodun [Ligand Id: 12003] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3769414 (IC-200214, IC200214, Iti-214, ITI-214, ITI-214F, Iti-214 free base, Lenrispodun)
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 1B in Human [GtoPdb: 1295] [UniProtKB: Q01064]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
ChEMBL Inhibition of recombinant full lenght human PDE4A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay B 7.21 pKi 62 nM Ki J Med Chem (2016) 59: 1149-1164 [PMID:26789933]
GtoPdb - - 6.8 pIC50 160 nM IC50 J Med Chem (2016) 59: 1149-64 [PMID:26789933]
phosphodiesterase 1B in Human [GtoPdb: 1295] [UniProtKB: Q01064]
GtoPdb - - 10.24 pIC50 0.06 nM IC50 J Med Chem (2016) 59: 1149-64 [PMID:26789933]

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]