Target Validation Information
TTD ID T89529
Target Name PTPN1 messenger RNA (PTPN1 mRNA)
Type of Target
Successful
Drug Potency against Target 1,2,3,4,6-penta-O-galloyl-D-glucopyranose Drug Info IC50 = 4800 nM [26]
1,2-NAPHTHOQUINONE Drug Info IC50 = 1640 nM [2]
16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acid Drug Info IC50 = 7100 nM [6]
18alpha-Glycyrrhetic acid Drug Info IC50 = 15600 nM [8]
18beta-Glycyrrhetic acid Drug Info IC50 = 13800 nM [8]
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid Drug Info IC50 = 8100 nM [15]
24-hydroxyursolic acid Drug Info IC50 = 12800 nM [15]
3,9-Dihydroxy-4-prenyl-[6aR,11aR]pterocarpan Drug Info IC50 = 19500 nM [21]
3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenol Drug Info IC50 = 8600 nM [1]
3-epi-masilinic acid Drug Info IC50 = 14330 nM [23]
3-isopropyl-4-(phenylthio)naphthalene-1,2-dione Drug Info IC50 = 13660 nM [5]
3-oxoolean-12-en-27-oic acid Drug Info IC50 = 6800 nM [8]
3alpha,24-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 11700 nM [8]
3beta,6beta-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 12800 nM [8]
3beta-acetoxyolean-12-en-27-oic acid Drug Info IC50 = 8500 nM [8]
3beta-hydroxyolean-12-en-27-oic acid Drug Info IC50 = 5200 nM [8]
3beta-hydroxyurs-12-en-27-oic acid Drug Info IC50 = 4900 nM [8]
4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-ol Drug Info IC50 = 1190 nM [18]
4'-(2-butylbenzofuran-3-yl)biphenyl-4-ol Drug Info IC50 = 740 nM [18]
4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione Drug Info IC50 = 19590 nM [5]
5-deoxyabyssinin II Drug Info IC50 = 19200 nM [11]
Abyssinin I Drug Info IC50 = 18200 nM [11]
Abyssinin II Drug Info IC50 = 17300 nM [11]
Abyssinoflavanone VI Drug Info IC50 = 18900 nM [11]
Abyssinoflavanone VII Drug Info IC50 = 15700 nM [11]
Abyssinone-IV Drug Info IC50 = 16000 nM [9]
Abyssinone-VI-4-O-methyl ether Drug Info IC50 = 14800 nM [9]
ALBAFURAN A Drug Info IC50 = 9200 nM [22]
Augustic acid Drug Info IC50 = 4930 nM [23]
BURTTINONE Drug Info IC50 = 18900 nM [16]
CAULERPIN Drug Info IC50 = 3770 nM [7]
CHROMOTROPATE Drug Info IC50 = 9700 nM [3]
DYSIDINE Drug Info IC50 = 6700 nM [17]
ERTIPROTAFIB Drug Info IC50 = 1400 nM [12]
Erybreadin b Drug Info IC50 = 4200 nM [21]
Erybreadin C Drug Info IC50 = 7300 nM [21]
Erybreadin D Drug Info IC50 = 6400 nM [21]
Erysubin E Drug Info IC50 = 8800 nM [21]
ERYTHRIBYSSIN A Drug Info IC50 = 19300 nM [21]
EVANS BLUE Drug Info IC50 = 1300 nM [3]
FOLITENOL Drug Info IC50 = 7800 nM [21]
FORMYLCHROMONE Drug Info Ki = 4300 nM [24]
Isochroman mono-carboxylic acid Drug Info IC50 = 51.63 nM [24]
Isoxazolecarboxylic acid Drug Info Ki = 5700 nM [24]
Kuwanon J Drug Info IC50 = 2700 nM [22]
Kuwanon L Drug Info IC50 = 16900 nM [4]
Kuwanon R Drug Info IC50 = 8200 nM [22]
Kuwanon V Drug Info IC50 = 13800 nM [22]
LICOAGROCHACONE A Drug Info IC50 = 19100 nM [19]
LICOAGROCHALCONE A Drug Info IC50 = 16900 nM [11]
MASLINIC ACID Drug Info IC50 = 5930 nM [23]
Methyl 3beta-hydroxyolean-12-en-28-oate Drug Info IC50 = 14200 nM [8]
Methyl3beta-hydroxyolean-12-en-27-oate Drug Info IC50 = 16000 nM [8]
Mulberrofuran C Drug Info IC50 = 4900 nM [4]
Mulberrofuran D Drug Info IC50 = 4300 nM [22]
Mulberrofuran W Drug Info IC50 = 2700 nM [22]
NEORAUTENOL Drug Info IC50 = 7600 nM [21]
OHIOENSIN A Drug Info IC50 = 4300 nM [13]
Ohioensin C Drug Info IC50 = 7600 nM [13]
Ohioensin F Drug Info Ki = 1500 nM [13]
Ohioensin G Drug Info IC50 = 5600 nM [13]
OLEANOLIC_ACID Drug Info IC50 = 4200 nM [20]
Oleanonic acid Drug Info IC50 = 3500 nM [15]
Oxalylaminobenzoic acid Drug Info Ki = 18 nM [24]
PHELLIGRIDIN I Drug Info IC50 = 3000 nM [10]
Pomolic acid Drug Info IC50 = 3900 nM [15]
RK-682 Drug Info IC50 = 4400 nM [25]
Rotungenic acid Drug Info IC50 = 10900 nM [15]
Sanggenon C Drug Info IC50 = 2600 nM [4]
Sanggenon G Drug Info IC50 = 1600 nM [4]
SIGMOIDIN A Drug Info IC50 = 14400 nM [11]
SIGMOIDIN B Drug Info IC50 = 19400 nM [11]
Sigmoidin F Drug Info IC50 = 14200 nM [11]
Spathodic acid Drug Info IC50 = 18800 nM [15]
TRYPAN BLUE Drug Info IC50 = 3900 nM [3]
URSOLIC ACID Drug Info IC50 = 3600 nM [21]
USIMINE A Drug Info IC50 = 15000 nM [14]
USNIC ACID Drug Info IC50 = 16400 nM [14]
UVAOL Drug Info IC50 = 15600 nM [15]
Action against Disease Model ISIS 113715 Drug Info In cultured monkey hepatocytes, ISIS 113715 treatment dose-dependently reduced PTP-1B mRNA expression, with an IC 50 of less than 10 nM. [27]
References
REF 1 Molecular docking and high-throughput screening for novel inhibitors of protein tyrosine phosphatase-1B. J Med Chem. 2002 May 23;45(11):2213-21.
REF 2 Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1941-6.
REF 3 Evans Blue and other dyes as protein tyrosine phosphatase inhibitors. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1923-6.
REF 4 Protein tyrosine phosphatase 1B inhibitors from Morus root bark. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1426-9.
REF 5 Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1905-8.
REF 6 Inhibition of protein tyrosine phosphatase 1B by diterpenoids isolated from Acanthopanax koreanum. Bioorg Med Chem Lett. 2006 Jun 1;16(11):3061-4.
REF 7 Two novel aromatic valerenane-type sesquiterpenes from the Chinese green alga Caulerpa taxifolia. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2947-50.
REF 8 Protein tyrosine phosphatase 1B inhibitory activity of triterpenes isolated from Astilbe koreana. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3273-6.
REF 9 Protein tyrosine phosphatase-1B inhibitory activity of isoprenylated flavonoids isolated from Erythrina mildbraedii. J Nat Prod. 2006 Nov;69(11):1572-6.
REF 10 Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius. J Nat Prod. 2007 Feb;70(2):296-9.
REF 11 Isoprenylated flavonoids from the stem bark of Erythrina abyssinica. J Nat Prod. 2007 Jun;70(6):1039-42.
REF 12 2-O-carboxymethylpyrogallol derivatives as PTP1B inhibitors with antihyperglycemic activity. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5357-60.
REF 13 Ohioensins F and G: protein tyrosine phosphatase 1B inhibitory benzonaphthoxanthenones from the Antarctic moss Polytrichastrum alpinum. Bioorg Med Chem Lett. 2008 Jan 15;18(2):772-5.
REF 14 Usimines A-C, bioactive usnic acid derivatives from the Antarctic lichen Stereocaulon alpinum. J Nat Prod. 2008 Apr;71(4):710-2.
REF 15 Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B. J Nat Prod. 2008 Oct;71(10):1775-8.
REF 16 Flavanones from the stem bark of Erythrina abyssinica. Bioorg Med Chem. 2008 Dec 15;16(24):10356-62.
REF 17 A novel sesquiterpene quinone from Hainan sponge Dysidea villosa. Bioorg Med Chem Lett. 2009 Jan 15;19(2):390-2.
REF 18 Synthesis, activity and molecular modeling of a new series of chromones as low molecular weight protein tyrosine phosphatase inhibitors. Bioorg Med Chem. 2009 Apr 1;17(7):2658-72.
REF 19 Inhibitory effect of chalcones and their derivatives from Glycyrrhiza inflata on protein tyrosine phosphatase 1B. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5155-7.
REF 20 Chemical Constituents of the Roots of Euphorbia micractina. J Nat Prod. 2009 Sep;72(9):1620-6.
REF 21 Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6745-9.
REF 22 Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6759-61.
REF 23 Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6618-22.
REF 24 Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents. Eur J Med Chem. 2010 Sep;45(9):3709-18.
REF 25 Prenylflavonoids from Glycyrrhiza uralensis and their protein tyrosine phosphatase-1B inhibitory activities. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5398-401.
REF 26 Bioactivity-guided isolation of 1,2,3,4,6-Penta-O-galloyl-D-glucopyranose from Paeonia lactiflora roots as a PTP1B inhibitor. J Nat Prod. 2010 Sep 24;73(9):1578-81.
REF 27 Inhibition of protein tyrosine phosphatase-1B with antisense oligonucleotides improves insulin sensitivity and increases adiponectin concentrations in monkeys. Endocrinology. 2009 Apr;150(4):1670-9.

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