ChEMBL ligand: CHEMBL1829872
Dual specificity protein phosphatase 22 in Human [ChEMBL: CHEMBL3924] [UniProtKB: Q9NRW4] There should be some charts here, you may need to enable JavaScript!
Papain in Carica papaya [ChEMBL: CHEMBL4779] [UniProtKB: P00784] There should be some charts here, you may need to enable JavaScript!
RTP Type S/Receptor-type tyrosine-protein phosphatase S in Human [ChEMBL: CHEMBL2396508] [GtoPdb: 1866] [UniProtKB: Q13332] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
protein tyrosine phosphatase non-receptor type 1/Tyrosine-protein phosphatase non-receptor type 1 in Human [ChEMBL: CHEMBL335] [GtoPdb: 2976] [UniProtKB: P18031] There should be some charts here, you may need to enable JavaScript!
protein tyrosine phosphatase non-receptor type 2/Tyrosine-protein phosphatase non-receptor type 2 in Human [ChEMBL: CHEMBL3807] [GtoPdb: 3255] [UniProtKB: P17706] 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
Dual specificity protein 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
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]
ChEMBL	Chromatin Immunoprecipitation (CHIP): ChIP assay was performed using EZ ChIP Kit (Millipore, Billerica, Mass., USA) as per manufacturer's instruction. Briefly, after crosslinking with formaldehyde (1%), cell were lysed using SDS Lysis Buffer containing Protease Inhibitor Cocktail and nuclear extract were obtained. Then, crosslinked DNA was sheared using sonication; sheared DNA size was checked on agarose gel and ranged, in all cases, between 300-500 bp. An amount of 1/20 of the shared chromatin was kept as an input. Sheared chromatin was incubated with rabbit polyclonal Phospho-Stat5 (Tyr694) Antibody (Cell Signaling, Danvers, Mass., USA) at dilution 1:50 or rabbit polyclonal IgG at appropriate concentration. Incubation was performed at 4° C. overnight. The antibody/chromatin complex was precipitated using Protein G Agarose beads. After elution, the crosslink of protein/DNA was reversed, and DNA was purified using Spin Columns. PCR was performed using platinum Taq (Invitrogen Canada, Burlington, ON, Canada). Two sets of primers were designed to amplify two DNA segments that contain STAT5-binding sites located 1672 bp and 428 bp upstream the start sites of C-Myc and Cyclin-D1, respectively. The STAT5-binding site in the C-MYC promoter is characterized by a 4N spacer and has the sequence (ttcccccgaa), whereas the one in the Cyclin D1 promoter is characterized by a 3N spacer and has the sequence (ttcttggaa).	B	4.54	pIC50	28800	nM	IC50	US-10196373-B2. Substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs as inhibitors of STAT protein (2019)
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 1/Tyrosine-protein phosphatase non-receptor type 1 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
protein tyrosine phosphatase non-receptor type 2/Tyrosine-protein phosphatase non-receptor type 2 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 36:

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]