Target Poor or Non Binder(s) Information

Target General Information

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Target ID

T12541

Target Info

Target Name

Phosphatidylinositol-4-kinase beta (PI4KB)

Synonyms

PtdIns 4-kinase beta; Phosphatidylinositol 4-kinase beta; PIK4CB; PI4Kbeta; PI4K92; PI4K-beta; NPIK

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Target Type

Clinical trial Target

Gene Name

PI4KB

UniProt ID

Q9UBF8

Poor Binders of This Target (in total, 20 binders)

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Compound Name

8-[(2R)-1-(3,5-Difluorophenyl)pyrrolidin-2-yl]-6-(morpholine-4-carbonyl)-2-morpholino-chromen-4-one

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Investigative

Compound Info

Synonyms

CHEMBL4060768; SCHEMBL13276616; HY-101517; CS-0021620

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Activity

IC50 ~ 50000 nM

[1]

Compound Name

3-(3-Bromo-5-methoxyphenyl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

SCHEMBL3607978; CHEMBL1242200; 3-(3-bromo-5-methoxyphenyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-[4-Amino-1-(2-piperidin-3-ylethyl)pyrazolo[3,4-d]pyrimidin-3-yl]-2-chlorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241943

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-[4-Amino-1-[(3R)-pyrrolidin-3-yl]pyrazolo[3,4-d]pyrimidin-3-yl]-2-fluorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1242658

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-methyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenol

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Investigative

Compound Info

Synonyms

CHEMBL1241301

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((R)-tetrahydrofuran-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-chlorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241768

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-methyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methylphenol

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Investigative

Compound Info

Synonyms

CHEMBL1241271

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Activity

IC50 = 100000 nM

[2]

Compound Name

1-Isopropyl-3-(pyrimidin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

SCHEMBL3616915; CHEMBL1241391; US9765037, Compound 18; BDBM340891; 1-propan-2-yl-3-pyrimidin-5-ylpyrazolo[3,4-d]pyrimidin-4-amine; 1-isopropyl-3-(pyrimidin-5-yl)-1H-pyrazolo[3,4- d]pyrimidin-4-amine

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((piperidin-4-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-chloropheno

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Investigative

Compound Info

Synonyms

CHEMBL1241859

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-fluorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1242845

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Activity

IC50 = 100000 nM

[2]

Compound Name

1-Cyclohexyl-3-(4-ethoxy-3-methoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

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Investigative

Compound Info

Synonyms

CHEMBL1242659

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenol

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Investigative

Compound Info

Synonyms

CHEMBL1242201

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((pyrrolidin-3-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-chlorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241770

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((piperidin-4-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-fluorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1242844

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Activity

IC50 = 100000 nM

[2]

Compound Name

Tert-butyl 5-(4-amino-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indole-1-carboxylate

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Investigative

Compound Info

Synonyms

SCHEMBL3604275; CHEMBL1242853; tert-butyl 5-(4-amino-1-cyclopentylpyrazolo[3,4-d]pyrimidin-3-yl)indole-1-carboxylate

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((piperidin-3-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-chlorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241858

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-ethyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenol

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Investigative

Compound Info

Synonyms

CHEMBL1242113

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((pyrrolidin-2-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-chlorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241769

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((4-phenyloxazol-5-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-fluorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1241482

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Activity

IC50 = 100000 nM

[2]

Compound Name

5-(4-Amino-1-((S)-pyrrolidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-fluorophenol

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Investigative

Compound Info

Synonyms

CHEMBL1242657

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Activity

IC50 = 100000 nM

[2]

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References

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REF 1

Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K/ inhibitors for the treatment of PTEN-deficient tumours. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954.

REF 2

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.

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