Target
Signal transducer and activator of transcription 3
Ligand
BDBM20208
Substrate
BDBM20194
Meas. Tech.
Fluorescence Polarization Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
>100000±n/a nM
Citation
 Coleman, DRRen, ZMandal, PKCameron, AGDyer, GAMuranjan, SCampbell, MChen, XMcMurray, JS Investigation of the binding determinants of phosphopeptides targeted to the SRC homology 2 domain of the signal transducer and activator of transcription 3. Development of a high-affinity peptide inhibitor. J Med Chem 48:6661-70 (2005) [PubMed]  Article 
Target
Name:
Signal transducer and activator of transcription 3
Synonyms:
Acute-phase response factor | Aprf | STAT3 alpha | STAT3_MOUSE | Signal transducer and activator of transcription 3 | Stat3 | Transcription Factor STAT3
Type:
Cytosolic Transcription Factor
Mol. Mass.:
88050.28
Organism:
Mus musculus (mouse)
Description:
Bacterially expressed protein was used in the FP assay.
Residue:
770
Sequence:
MAQWNQLQQLDTRYLEQLHQLYSDSFPMELRQFLAPWIESQDWAYAASKESHATLVFHNLLGEIDQQYSRFLQESNVLYQHNLRRIKQFLQSRYLEKPMEIARIVARCLWEESRLLQTAATAAQQGGQANHPTAAVVTEKQQMLEQHLQDVRKRVQDLEQKMKVVENLQDDFDFNYKTLKSQGDMQDLNGNNQSVTRQKMQQLEQMLTALDQMRRSIVSELAGLLSAMEYVQKTLTDEELADWKRRQQIACIGGPPNICLDRLENWITSLAESQLQTRQQIKKLEELQQKVSYKGDPIVQHRPMLEERIVELFRNLMKSAFVVERQPCMPMHPDRPLVIKTGVQFTTKVRLLVKFPELNYQLKIKVCIDKDSGDVAALRGSRKFNILGTNTKVMNMEESNNGSLSAEFKHLTLREQRCGNGGRANCDASLIVTEELHLITFETEVYHQGLKIDLETHSLPVVVISNICQMPNAWASILWYNMLTNNPKNVNFFTKPPIGTWDQVAEVLSWQFSSTTKRGLSIEQLTTLAEKLLGPGVNYSGCQITWAKFCKENMAGKGFSFWVWLDNIIDLVKKYILALWNEGYIMGFISKERERAILSTKPPGTFLLRFSESSKEGGVTFTWVEKDISGKTQIQSVEPYTKQQLNNMSFAEIIMGYKIMDATNILVSPLVYLYPDIPKEEAFGKYCRPESQEHPEADPGSAAPYLKTKFICVTPTTCSNTIDLPMSPRTLDSLMQFGNNGEGAEPSAGGQFESLTFDMDLTSECATSPM
  
Inhibitor
Name:
BDBM20208
Synonyms:
15, Ac-pTyr-Leu-D-Pro-Gln-Thr-NH2 | 4-[(2S)-2-{[(2S)-1-[(2R)-2-{[(1S)-3-carbamoyl-1-{[(1S,2S)-1-carbamoyl-2-hydroxypropyl]carbamoyl}propyl]carbamoyl}pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]carbamoyl}-2-acetamidoethyl]phenoxyphosphonic acid
Type:
Phosphopeptide
Emp. Form.:
C31H48N7O12P
Mol. Mass.:
741.7263
SMILES:
CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OP(O)(O)=O)cc1)NC(C)=O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)O)C(N)=O |r|
Structure:
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Substrate
Name:
BDBM20194
Synonyms:
5-carboxyfluoresceinyl-Ala-Tyr(PO3H2)-Leu-Pro-Gln-Thr-Val-NH2 | 5-{[(1S)-1-{[(1S)-1-{[(2S)-1-[(2S)-2-{[(1S)-3-carbamoyl-1-{[(1S,2S)-1-{[(1S)-1-carbamoyl-2-methylpropyl]carbamoyl}-2-hydroxypropyl]carbamoyl}propyl]carbamoyl}pyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]carbamoyl}-2-[4-(phosphonooxy)phenyl]ethyl]carbamoyl}ethyl]carbamoyl}-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid | Ala-Tyr(PO3H2)-Leu-Pro-Gln-Thr-Val-NH2
Type:
Fluorescent Peptide
Emp. Form.:
C58H70N9O19P
Mol. Mass.:
1228.1991
SMILES:
CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(OP(O)(O)=O)cc1)NC(=O)[C@H](C)NC(=O)c1ccc(c(c1)C(O)=O)-c1c2ccc(O)cc2oc2cc(=O)ccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C(C)O)C(=O)N[C@@H](C(C)C)C(N)=O |r,wU:8.21,64.69,80.85,wD:24.25,4.4,60.66,73.78,(10.21,-4.51,;9.44,-3.18,;7.9,-3.18,;10.21,-1.85,;10.21,-.31,;8.88,.46,;7.54,-.31,;7.54,-1.85,;6.21,.46,;6.21,2,;5.44,3.34,;3.9,3.22,;3.03,4.49,;3.7,5.88,;2.61,6.96,;3.38,8.3,;4.15,9.63,;4.92,8.3,;2.29,9.39,;5.23,6,;6.1,4.73,;4.88,-.31,;3.54,.46,;3.54,2,;2.21,-.31,;2.01,-1.83,;1.12,.78,;.35,2.12,;1.12,3.45,;-1.19,2.12,;-1.96,.78,;-3.5,.78,;-4.27,2.12,;-3.5,3.45,;-1.96,3.45,;-3.9,4.94,;-2.81,6.03,;-5.39,5.34,;-5.81,2.12,;-6.58,3.45,;-5.81,4.78,;-6.58,6.12,;-8.12,6.12,;-8.89,7.45,;-8.89,4.78,;-8.12,3.45,;-8.89,2.12,;-8.12,.78,;-8.89,-.55,;-8.12,-1.88,;-8.89,-3.22,;-6.58,-1.88,;-5.81,-.55,;-6.58,.78,;11.54,.46,;11.54,2,;12.88,-.31,;12.83,-1.85,;14.28,-2.36,;15.22,-1.15,;14.36,.13,;15.13,1.46,;14.36,2.79,;16.46,.69,;17.79,1.46,;17.79,3,;19.13,3.77,;19.13,5.31,;20.46,6.08,;17.79,6.08,;19.13,.69,;19.13,-.85,;20.46,1.46,;21.79,.69,;21.79,-.85,;20.46,-1.62,;23.13,-1.62,;23.13,1.46,;23.13,3,;24.46,.69,;25.8,1.46,;25.8,3,;24.46,3.77,;27.13,3.77,;27.13,.69,;28.46,1.46,;27.13,-.85,)|
Structure:
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