Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T23787 | Target Info | |||
| Target Name | Renal carcinoma antigen NY-REN-56 (PFKFB3) | ||||
| Synonyms |
iPFK2; Renal carcinoma antigen NYREN56; PFKFB3; Fructose2,6bisphosphatase; 6phosphofructo2kinase/fructose2,6bisphosphatase 3; 6PF2K/Fru2,6P2ase brain/placentatype isozyme; 6PF2K/Fru2,6P2ase 3
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| Target Type | Clinical trial Target | ||||
| Gene Name | PFKFB3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Ethyl 1-[5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-6-oxo-1-phenylpyridazin-4-yl]triazole-4-carboxylate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105825; BDBM50445934
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| Activity |
IC50 = 55000 nM
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[1] | |||
| Compound Name |
Schembl21856796
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3422665; BDBM50082197
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| Activity |
IC50 = 70900 nM
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[2] | |||
| Compound Name |
5-(4-Acetylaminophenoxy)-2-amino-1H-indole-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3422655; PFKFB3-IN-1; SCHEMBL5857153; N-[4-[(2-amino-3-cyano-1H-indol-5-yl)oxy]phenyl]acetamide; BDBM50082131
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
(2R)-2-Amino-N-[4-[(2-amino-3-cyano-1H-indol-5-yl)oxy]phenyl]-3-hydroxypropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3421643; BDBM50082129
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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Investigative | Compound Info | ||
| Synonyms |
(E)-3PO; CHEMBL3105848; (E)-3-(Pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one; SCHEMBL196639; (E)-3PO;3PO; BCP34641; ZINC3997313; BDBM50445948; s7639; 3PO, >=98% (HPLC); AKOS025142053; CCG-266648; CS-5491; SB17190; NCGC00386709-03; AS-55969; HY-19824; AB00079158-01; SR-01000203323; SR-01000203323-1; 2-Propen-1-one, 3-(3-pyridinyl)-1-(4-pyridinyl)-; 3-(pyridin-3-yl)-1-(pyridin-4-yl)prop-2-en-1-one; (2E)-3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one; (E)-3-pyridin-3-yl-1-pyridin-4-ylprop-2-en-1-one (3PO); (2E)-3-(PYRIDIN-3-YL)-1-(PYRIDIN-4-YL)PROP-2-EN-1-ONE
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Non Binders of This Target (in total, 11 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-(5-Bromo-6-oxo-1-phenylpyridazin-4-yl)-3,4-dihydro-1H-isoquinoline-5-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105840; BDBM50445942
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| Activity |
IC50 > 500000 nM
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[1] | |||
| Compound Name |
5-(4-Acetyl-5-methyltriazol-1-yl)-4-bromo-2-[[4-[2-(dimethylamino)ethylamino]phenyl]methyl]pyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105835; BDBM50445949
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| Activity |
IC50 > 500000 nM
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[1] | |||
| Compound Name |
5-(4-Acetyl-5-methyltriazol-1-yl)-2-phenyl-4-propan-2-ylpyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105846; BDBM50445936
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| Activity |
IC50 > 500000 nM
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[1] | |||
| Compound Name |
1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
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Investigative | Compound Info | ||
| Synonyms |
PFK-015; PFK15; CHEMBL3105836; (E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one; 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one; PFK 15; PFK015; SCHEMBL2702934; SCHEMBL16534534; AOB4632; SYN5216; BCP10875; EX-A4218; 2649AH; BDBM50445946; s7289; AKOS025287166; ZINC103235314; ACN-050165; CCG-267056; NCGC00386328-09; AC-28651; AS-16574; HY-12204; SW219876-1; A14287; (E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
4-Bromo-5-(morpholin-4-yl)-2-phenylpyridazin-3(2H)-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1463854; 4-bromo-5-morpholin-4-yl-2-phenylpyridazin-3(2H)-one; ChemDiv3_005468; MLS000727518; HMS1488I12; HMS2685L20; ZINC147920; BDBM50445943; STK172347; AKOS000425513; CCG-115604; MCULE-9052925903; IDI1_023378; SMR000306215; SR-01000085561; SR-01000085561-1; BRD-K45989580-001-01-2; Z57347150; 4-bromo-5-(morpholin-4-yl)-2-phenyl-2,3-dihydropyridazin-3-one
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
4-Bromo-5-(oxolan-2-ylmethylamino)-2-phenylpyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105843; BDBM50445939
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
2-[(5-Bromo-6-oxo-1-phenylpyridazin-4-yl)amino]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105842; BDBM50445940
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
4-Bromo-5-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-2-phenylpyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105841; BDBM50445941
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| Activity |
IC50 > 1000000 nM
|
[1] | |||
| Compound Name |
3H-Benzo[e]indol-2-yl(pyridin-4-yl)methanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105837; SCHEMBL2302776; BDBM50445947
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
5-(4-Acetyl-5-methyltriazol-1-yl)-4-ethoxy-2-phenylpyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105847; BDBM50445935
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| Activity |
IC50 > 1000000 nM
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[1] | |||
| Compound Name |
5-(4-Acetyl-5-methyltriazol-1-yl)-2-benzylpyridazin-3-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3105831; BDBM50445928
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| Activity |
IC50 > 10000000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). Bioorg Med Chem. 2014 Feb 1;22(3):1029-39. | ||||
| REF 2 | Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3. J Med Chem. 2015 Apr 23;58(8):3611-25. | ||||
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