Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR01437
Target NamemRNA of Protein tyrosine phosphatase-1B    
Type of TargetResearch target    
Drug Potency against Targetrotungenic acidIC50 = 10900 nM[1]
3alpha,24-dihydroxyolean-12-en-27-oic acidIC50 = 11700 nM[2]
4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-olIC50 = 1190 nM[3]
24-hydroxyursolic acidIC50 = 12800 nM[1]
3beta,6beta-dihydroxyolean-12-en-27-oic acidIC50 = 12800 nM[2]
EVANS BLUEIC50 = 1300 nM[4]
3-isopropyl-4-(phenylthio)naphthalene-1,2-dioneIC50 = 13660 nM[5]
18beta-Glycyrrhetic acidIC50 = 13800 nM[2]
kuwanon VIC50 = 13800 nM[6]
ERTIPROTAFIBIC50 = 1400 nM[7]
methyl 3beta-hydroxyolean-12-en-28-oateIC50 = 14200 nM[2]
sigmoidin FIC50 = 14200 nM[8]
3-epi-masilinic acidIC50 = 14330 nM[9]
SIGMOIDIN AIC50 = 14400 nM[8]
abyssinone-VI-4-O-methyl etherIC50 = 14800 nM[10]
USIMINE AIC50 = 15000 nM[11]
18alpha-Glycyrrhetic acidIC50 = 15600 nM[2]
UVAOLIC50 = 15600 nM[1]
abyssinoflavanone VIIIC50 = 15700 nM[8]
Sanggenon GIC50 = 1600 nM[12]
abyssinone-IVIC50 = 16000 nM[10]
methyl3beta-hydroxyolean-12-en-27-oateIC50 = 16000 nM[2]
1,2-NAPHTHOQUINONEIC50 = 1640 nM[13]
USNIC ACIDIC50 = 16400 nM[11]
Kuwanon LIC50 = 16900 nM[12]
LICOAGROCHALCONE AIC50 = 16900 nM[8]
abyssinin IIIC50 = 17300 nM[8]
abyssinin IIC50 = 18200 nM[8]
spathodic acidIC50 = 18800 nM[1]
BURTTINONEIC50 = 18900 nM[14]
abyssinoflavanone VIIC50 = 18900 nM[8]
LICOAGROCHACONE AIC50 = 19100 nM[15]
5-deoxyabyssinin IIIC50 = 19200 nM[8]
ERYTHRIBYSSIN AIC50 = 19300 nM[16]
SIGMOIDIN BIC50 = 19400 nM[8]
3,9-Dihydroxy-4-prenyl-[6aR;11aR]pterocarpanIC50 = 19500 nM[16]
4-(p-toluidino)-3-isopropylnaphthalene-1,2-dioneIC50 = 19590 nM[5]
Sanggenon CIC50 = 2600 nM[12]
mulberrofuran WIC50 = 2700 nM[6]
kuwanon JIC50 = 2700 nM[6]
PHELLIGRIDIN IIC50 = 3000 nM[17]
oleanonic acidIC50 = 3500 nM[1]
URSOLIC ACIDIC50 = 3600 nM[16]
CAULERPINIC50 = 3770 nM[18]
TRYPAN BLUEIC50 = 3900 nM[4]
pomolic acidIC50 = 3900 nM[1]
ERYBREADIN BIC50 = 4200 nM[16]
OLEANOLIC_ACIDIC50 = 4200 nM[19]
OHIOENSIN AIC50 = 4300 nM[20]
mulberrofuran DIC50 = 4300 nM[6]
RK-682IC50 = 4400 nM[21]
1,2,3,4,6-penta-O-galloyl-D-glucopyranoseIC50 = 4800 nM[22]
3beta-hydroxyurs-12-en-27-oic acidIC50 = 4900 nM[2]
Mulberrofuran CIC50 = 4900 nM[12]
augustic acidIC50 = 4930 nM[9]
isochroman mono-carboxylic acidIC50 = 51.63 nM[23]
3beta-hydroxyolean-12-en-27-oic acidIC50 = 5200 nM[2]
ohioensin GIC50 = 5600 nM[20]
MASLINIC ACIDIC50 = 5930 nM[9]
Erybreadin DIC50 = 6400 nM[16]
DYSIDINEIC50 = 6700 nM[24]
3-oxoolean-12-en-27-oic acidIC50 = 6800 nM[2]
16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acidIC50 = 7100 nM[25]
Erybreadin CIC50 = 7300 nM[16]
4'-(2-butylbenzofuran-3-yl)biphenyl-4-olIC50 = 740 nM[3]
NEORAUTENOLIC50 = 7600 nM[16]
ohioensin CIC50 = 7600 nM[20]
FOLITENOLIC50 = 7800 nM[16]
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acidIC50 = 8100 nM[1]
kuwanon RIC50 = 8200 nM[6]
3beta-acetoxyolean-12-en-27-oic acidIC50 = 8500 nM[2]
3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenolIC50 = 8600 nM[26]
Erysubin EIC50 = 8800 nM[16]
ALBAFURAN AIC50 = 9200 nM[6]
CHROMOTROPATEIC50 = 9700 nM[4]
ohioensin FKi = 1500 nM[20]
oxalylaminobenzoic acidKi = 18 nM[23]
FORMYLCHROMONEKi = 4300 nM[23]
isoxazolecarboxylic acidKi = 5700 nM[23]
Ref 1J Nat Prod. 2008 Oct;71(10):1775-8. Epub 2008 Sep 18.Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B. To Reference
Ref 2Bioorg Med Chem Lett. 2006 Jun 15;16(12):3273-6. Epub 2006 Mar 31.Protein tyrosine phosphatase 1B inhibitory activity of triterpenes isolated from Astilbe koreana. To Reference
Ref 3Bioorg Med Chem. 2009 Apr 1;17(7):2658-72. Epub 2009 Mar 5.Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors. To Reference
Ref 4Bioorg Med Chem Lett. 2004 Apr 19;14(8):1923-6.Evans Blue and other dyes as protein tyrosine phosphatase inhibitors. To Reference
Ref 5Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8. Epub 2006 Jan 24.Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases. To Reference
Ref 6Bioorg Med Chem Lett. 2009 Dec 1;19(23):6759-61. Epub 2009 Oct 7.Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis. To Reference
Ref 7Bioorg Med Chem Lett. 2007 Oct 1;17(19):5357-60. Epub 2007 Aug 15.2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity. To Reference
Ref 8J Nat Prod. 2007 Jun;70(6):1039-42. Epub 2007 May 10.Isoprenylated flavonoids from the stem bark of Erythrina abyssinica. To Reference
Ref 9Bioorg Med Chem Lett. 2009 Dec 1;19(23):6618-22. Epub 2009 Oct 8.Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B. To Reference
Ref 10J Nat Prod. 2006 Nov;69(11):1572-6.Protein tyrosine phosphatase-1B inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii. To Reference
Ref 11J Nat Prod. 2008 Apr;71(4):710-2. Epub 2008 Feb 21.Usimines A-C, bioactive usnic acid derivatives from the Antarctic lichen Stereocaulon alpinum. To Reference
Ref 12Bioorg Med Chem Lett. 2006 Mar 1;16(5):1426-9. Epub 2005 Dec 13.Protein tyrosine phosphatase 1B inhibitors from Morus root bark. To Reference
Ref 13Bioorg Med Chem Lett. 2002 Aug 5;12(15):1941-6.Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents. To Reference
Ref 14Bioorg Med Chem. 2008 Dec 15;16(24):10356-62. Epub 2008 Oct 10.Flavanones from the stem bark of Erythrina abyssinica. To Reference
Ref 15Bioorg Med Chem Lett. 2009 Sep 1;19(17):5155-7. Epub 2009 Jul 24.Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B. To Reference
Ref 16Bioorg Med Chem Lett. 2009 Dec 1;19(23):6745-9. Epub 2009 Oct 1.Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica. To Reference
Ref 17J Nat Prod. 2007 Feb;70(2):296-9. Epub 2007 Feb 6.Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius. To Reference
Ref 18Bioorg Med Chem Lett. 2006 Jun 1;16(11):2947-50. Epub 2006 Mar 24.Two novel aromatic valerenane-type sesquiterpenes from the Chinese green alga Caulerpa taxifolia. To Reference
Ref 19J Nat Prod. 2009 Sep;72(9):1620-6.Chemical Constituents of the Roots of Euphorbia micractina. To Reference
Ref 20Bioorg Med Chem Lett. 2008 Jan 15;18(2):772-5. Epub 2007 Nov 17.Ohioensins F and G: protein tyrosine phosphatase 1B inhibitory benzonaphthoxanthenones from the Antarctic moss Polytrichastrum alpinum. To Reference
Ref 21Bioorg Med Chem Lett. 2010 Sep 15;20(18):5398-401. Epub 2010 Aug 1.Prenylflavonoids from Glycyrrhiza uralensis and their protein tyrosine phosphatase-1B inhibitory activities. To Reference
Ref 22J Nat Prod. 2010 Sep 24;73(9):1578-81.Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor. To Reference
Ref 23Eur J Med Chem. 2010 Sep;45(9):3709-18. Epub 2010 May 15.Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents. To Reference
Ref 24Bioorg Med Chem Lett. 2009 Jan 15;19(2):390-2. Epub 2008 Nov 24.A novel sesquiterpene quinone from Hainan sponge Dysidea villosa. To Reference
Ref 25Bioorg Med Chem Lett. 2006 Jun 1;16(11):3061-4. Epub 2006 Mar 20.Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum. To Reference
Ref 26J Med Chem. 2002 May 23;45(11):2213-21.Molecular docking and high-throughput screening for novel inhibitors of protein tyrosine phosphatase-1B. To Reference



 

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