Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T39231 | Target Info | |||
| Target Name | Tankyrase-1 (TNKS-1) | ||||
| Synonyms |
Tankyrase I; TRF1-interacting ankyrin-related ADP-ribose polymerase; TNKS1; TINF1; TIN1; TANK1; Protein poly-ADP-ribosyltransferase tankyrase-1; Poly [ADP-ribose] polymerase tankyrase-1; Poly [ADP-ribose] polymerase 5A; PARPL; PARP5A; ARTD5; ADP-ribosyltransferase diphtheria toxin-like 5
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| Target Type | Clinical trial Target | ||||
| Gene Name | TNKS | ||||
| Biochemical Class | Glycosyltransferases | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 15 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-(2-Methylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4105641
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| Activity |
IC50 = 63095.73 nM
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[1] | |||
| Compound Name |
4-[(1S,2R,6S,7R)-4-Azatricyclo[5.2.1.02,6]dec-8-en-4-yl]-N-quinolin-8-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2431798
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| Activity |
IC50 = 64000 nM
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[2] | |||
| Compound Name |
4-(4-Carbamoylphenoxy)benzamide
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Investigative | Compound Info | ||
| Synonyms |
4,4'-oxydibenzamide; OUL35; 4,4'-Oxybis[benzamide]; MLS000736992; 4-(4-aminocarbonylphenoxy)benzamide; NSC39047; Oprea1_001354; IFLab1_001185; OUL 35; SCHEMBL3137816; CHEMBL1438938; CTK5B8808; DTXSID10284793; BDBM199181; HMS1415F19; HMS2754A23; ZINC235625; NSC-39047; AKOS001482413; MCULE-8450176580; IDI1_009052; OUL35, >=98% (HPLC); SMR000393949; EU-0000374; SR-01000391101; SR-01000391101-1; 4-[(4-Carbamoylcyclohexyl)oxy]cyclohexane-1-carboxamide (OUL35)
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
3-(8-Methyl-4-oxo-1H-quinazolin-2-yl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4080163; SCHEMBL19953233; BDBM50234917
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
4H-Thieno[2,3-c]isoquinolin-5-one
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Investigative | Compound Info | ||
| Synonyms |
TIQ-A; Thieno[2,3-c]isoquinolin-5(4H)-one; CHEMBL3108871; 4H,5H-thieno[2,3-c]isoquinolin-5-one; PARP Inhibitor X, TIQ-A; Thieno[2,3-c]isoquinolin-5-one; SCHEMBL422013; ZINC3266; CTK1C8658; DTXSID10432530; BDBM50446131; MFCD06407947; AKOS026417830; TIQ-A, >=98% (HPLC), solid; NE35457; NCGC00165904-01; DA-42468; FT-0675250; Q27460510; Z1889917149
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
4-(4-Formyl-phenoxy)-benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4287655; 4-(4-Formylphenoxy)-benzamide; 4-(4-formylphenoxy)benzamide; SCHEMBL754740; BDBM50468581; ZINC20297191; A1-11748
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
4-Methoxybenzamide
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Investigative | Compound Info | ||
| Synonyms |
p-Anisamide; p-Methoxybenzamide; 4-Methoxy benzamide; Benzamide, 4-methoxy-; 4-methoxy-benzamide; UNII-Z85FX3977E; CHEMBL449635; Z85FX3977E; MFCD00007995; 4-Methoxybenzamide, 97%; P-methyoxybenzamide; EINECS 222-319-6; BRN 1862847; ACMC-1CJJO; 4-Methoxybenzamide, 98%; Oprea1_456315; 4-10-00-00433 (Beilstein Handbook Reference); KSC225C6N; SCHEMBL201761; SCHEMBL12015238; CTK1C5166; KS-00000FKR; DTXSID40879434; ZINC161203; ACT03272; NSC11139; ANW-27812; BDBM50340090; NSC-11139; STL482885; AKOS000266484; AB00908; CS-W022205; GS-6794; MCULE-3713623573; VZ29332; AC-17055; AK114264; SC-65292; AB0016899; DB-006861; FT-0600843; M1679; ST50824264; 24M939; W-2595; W-106742; Q20059730; Z33546492
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
Chembl4125748
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Investigative | Compound Info | ||
| Synonyms |
BDBM50272959
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| Activity |
IC50 ~ 100000 nM
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[6] | |||
| Compound Name |
4-[(2-Fluorophenyl)methoxy]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4208737; OUL35 derivative 32; SCHEMBL20883219; 4-[(2-fluorobenzyl)oxy]benzamide; ZINC7509736; BDBM50452662; STL506080; AKOS017030557; MCULE-5507437194; Z26312097
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
2-[(Dimethylamino)methyl]-4H-thieno[2,3-c]isoquinolin-5-one;hydrochloride
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL4326979; CHEMBL3219282
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
2-Dimethylaminomethyl-9-hydroxythieno[2,3-c]isoquinolin-5(4H)-one hydrobromide
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL1549763; CHEMBL3219283; 2-dimethylaminomethyl-9-hydroxy-4h-thieno[2,3-c]isoquinolin-5-one-hydrobromide
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| Activity |
IC50 ~ 100000 nM
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[5] | |||
| Compound Name |
3-(4-Oxo-3,4-dihydroquinazolin-2-yl)propanoic acid
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Investigative | Compound Info | ||
| Synonyms |
3-(4-oxo-1H-quinazolin-2-yl)propanoic acid; 3-(4-Oxo-3,4-dihydro-quinazolin-2-yl)-propionic acid; 3,4-Dihydro-4-oxo-; CHEMBL1892587; NSC251919; Enamine_004755; 2-Quinazolinepropanoic acid, 1,4-dihydro-4-oxo-; MLS000775861; SCHEMBL2718160; SCHEMBL19953232; CTK1H2249; DTXSID00312256; HMS1407I03; HMS2754F07; ALBB-030898; ZINC1556709; BBL030181; BDBM50234922; MFCD03955531; STL374134; STL521303; AKOS000669520; AKOS005202394; AKOS028111280; MCULE-9759862525; NSC-251919; 2-(2-carboxyethyl)quinazolin-4(3h)-one; BS-14054; DA-42158; SMR000370984; 3-(4-hydroxyquinazolin-2-yl)propanoicacid; BB 0304036; FT-0667036; EN300-04546; SR-01000353582; 3-(4-HYDROXYQUINAZOLIN-2-YL)PROPANOIC ACID; SR-01000353582-1; 1,4-DIHYDRO-4-OXO-2-QUINAZOLINEPROPANOIC ACID; 3-(4-Oxo-1,4-dihydroquinazolin-2-yl)propanoic acid; Z56869288; 3-(4-oxo-3,4-dihydro-quinazolin-2-yl)-propionic acid, AldrichCPR
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
4-(4-Carbamoylphenoxy)benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4287262; BDBM50468579; ZINC20297208; AKOS009229962; MCULE-8977258216; NE43435; EN300-70101; Z1222331858
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
4-Amino-N-quinolin-8-ylbenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4063631; SCHEMBL15093487; CTK7D7163; ZINC4933157; BDBM50234918; AKOS000152295; 4-AMINO-N-(QUINOLIN-8-YL)BENZAMIDE
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
N-(3-Propan-2-ylphenyl)tetrazolo[1,5-a]quinoxalin-4-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4092054
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| Activity |
IC50 ~ 199526.23 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. J Med Chem. 2017 Jul 13;60(13):5455-5471. | ||||
| REF 2 | Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. J Med Chem. 2013 Oct 24;56(20):7880-9. | ||||
| REF 3 | 4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10. Eur J Med Chem. 2018 Aug 5;156:93-102. | ||||
| REF 4 | Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity. J Med Chem. 2017 Jan 26;60(2):814-820. | ||||
| REF 5 | Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ. Medchemcomm. 2011;2:559-65. | ||||
| REF 6 | Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2050-2054. | ||||
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