crisaborole [Ligand Id: 9151] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL484785 (AN2728, AN-2728, Crisaborole, Eucrisa)
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  • phosphodiesterase 1A/Phosphodiesterase 1A in Human [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
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  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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  • phosphodiesterase 7A/Phosphodiesterase 7A in Human [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Beta-lactamase in Klebsiella pneumoniae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641358] [UniProtKB: Q93LQ9]
ChEMBL Inhibition of Klebsiella pneumoniae KPC-2 B 6.17 pIC50 670 nM IC50 Bioorg Med Chem Lett (2021) 41: 127956-127956 [PMID:33744439]
phosphodiesterase 1A/Phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
GtoPdb - - 5.21 pIC50 6100 nM IC50 Bioorg Med Chem Lett (2009) 19: 2129-32 [PMID:19303290]
ChEMBL Inhibition of human recombinant PDE1A3 expressed in baculovirus-infected insect Sf9 cells by modified two-step method B 5.21 pIC50 6100 nM IC50 Bioorg Med Chem Lett (2009) 19: 2129-2132 [PMID:19303290]
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
ChEMBL Inhibition of PDE4A1A (unknown origin) B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 10375-10384 [PMID:30052440]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of PDE4B (unknown origin) B 4.15 pIC50 70000 nM IC50 Eur J Med Chem (2021) 213: 113171-113171 [PMID:33482600]
ChEMBL Inhibition of PDE4B (unknown origin) assessed as hydrolysis of [3H]-cGMP into [3H]-GMP incubated for 30 mins by scintillation of proximity assay B 7.24 pIC50 57.2 nM IC50 Eur J Med Chem (2021) 213: 113171-113171 [PMID:33482600]
ChEMBL Inhibition of PDE4B2 (unknown origin) B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 10375-10384 [PMID:30052440]
ChEMBL Inhibition of PDE4B1 (unknown origin) B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 10375-10384 [PMID:30052440]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
ChEMBL Inhibition of PDE4C1 (unknown origin) B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 10375-10384 [PMID:30052440]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of PDE4D7 (unknown origin) B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 10375-10384 [PMID:30052440]
phosphodiesterase 7A/Phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
ChEMBL Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method B 6.14 pIC50 730 nM IC50 Bioorg Med Chem Lett (2009) 19: 2129-2132 [PMID:19303290]
GtoPdb - - 6.14 pIC50 730 nM IC50 Bioorg Med Chem Lett (2009) 19: 2129-32 [PMID:19303290]

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]