compound 7b [Haftchenary et al., 2013] [Ligand Id: 8850] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1829872
  • Dual specificity phosphatase 22 in Human [ChEMBL: CHEMBL3924] [UniProtKB: Q9NRW4]
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  • protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
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  • RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332]
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  • signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763]
  • signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Mouse [ChEMBL: CHEMBL5402] [GtoPdb: 2994] [UniProtKB: P42227]
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  • protein tyrosine phosphatase non-receptor type 2/T-cell protein-tyrosine phosphatase in Human [ChEMBL: CHEMBL3807] [GtoPdb: 3255] [UniProtKB: P17706]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dual specificity phosphatase 22 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3924] [UniProtKB: Q9NRW4]
ChEMBL Inhibition of human GST-tagged full length MKPX assessed as DiFMUP hydrolysis by fluorometric kinetic-based assay B 5 pIC50 >10000 nM IC50 Medchemcomm (2013) 4: 987-992
Papain in Carica papaya (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4779] [UniProtKB: P00784]
ChEMBL Inhibition of papaya papain assessed as Z-Phe-Arg-pNA hydrolysis by fluorometric kinetic-based assay B 5 pIC50 >10000 nM IC50 Medchemcomm (2013) 4: 987-992
protein tyrosine phosphatase non-receptor type 1/Protein-tyrosine phosphatase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031]
ChEMBL Competitive inhibition of human GST-tagged PTP1B catalytic domain assessed as rate of DiFMUP hydrolysis by lineweaver-burk plot analysis B 5.4 pKi 4000 nM Ki Medchemcomm (2013) 4: 987-992
ChEMBL Inhibition of human GST-tagged PTP1B catalytic domain assessed as DiFMUP hydrolysis by fluorometric kinetic-based assay B 5.31 pIC50 4900 nM IC50 Medchemcomm (2013) 4: 987-992
GtoPdb - - 5.31 pIC50 4900 nM IC50 Medchemcomm (2013) : 987-992
RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332]
GtoPdb - - 5.44 pIC50 3600 nM IC50 Medchemcomm (2013) : 987-992
ChEMBL Inhibition of human GST-tagged PTP-sigma D1D2 domain assessed as DiFMUP hydrolysis by fluorometric kinetic-based assay B 5.44 pIC50 3600 nM IC50 Medchemcomm (2013) 4: 987-992
signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4026] [GtoPdb: 2994] [UniProtKB: P40763]
ChEMBL Inhibition of STAT3 using fluorescent probe 5-carboxyfluorescein-GpYLPQTV-NH2 after 15 mins by fluorescence polarisation assay B 4.88 pKi 13300 nM Ki Bioorg Med Chem Lett (2011) 21: 5605-5609 [PMID:21788134]
signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5402] [GtoPdb: 2994] [UniProtKB: P42227]
ChEMBL Inhibition of STAT3 in mouse NIH3T3/vSrc nuclear extract assessed as disruption of the Stat3-DNA complex pre-incubated for 30 mins by EMSA analysis B 4.54 pIC50 28800 nM IC50 Bioorg Med Chem Lett (2011) 21: 5605-5609 [PMID:21788134]
protein tyrosine phosphatase non-receptor type 2/T-cell protein-tyrosine phosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3807] [GtoPdb: 3255] [UniProtKB: P17706]
ChEMBL Inhibition of human GST-tagged TC-PTP catalytic domain assessed as DiFMUP hydrolysis by fluorometric kinetic-based assay B 5.29 pIC50 5100 nM IC50 Medchemcomm (2013) 4: 987-992

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]