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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL484785 (AN-2728, AN2728, Crisaborole, Eucrisa, Staquis)
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 1A/Phosphodiesterase 1A in Human [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 7A/Phosphodiesterase 7A in Human [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
There should be some charts here, you may need to enable JavaScript!
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 human PDE4 catalytic domain expressed in Escherichia coli B 6.96 pIC50 110 nM IC50 J Med Chem (2021) 64: 17706-17727 [PMID:34875836]
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 PDE4D (unknown origin) B 6.31 pIC50 490 nM IC50 J Med Chem (2022) 65: 4238-4254 [PMID:35188767]
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 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]