Target Poor or Non Binder(s) Information

Target General Information

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Target ID

T01283

Target Info

Target Name

Tumor susceptibility gene protein 101 (TSG101)

Synonyms

Tumor susceptibility gene 101 protein; ESCRT-I complex subunit TSG101

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Target Type

Clinical trial Target

Gene Name

TSG101

Biochemical Class

Ubiquitin-conjugating enzyme

UniProt ID

Q99816

Poor Binders of This Target (in total, 12 binders)

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Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-(4-phenylmethoxyphenyl)methylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL411538; BDBM50230484

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Activity

IC50 = 54000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4R)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-nonylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL403600; BDBM50230478

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Activity

IC50 = 54000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-2-[[(2S,4S)-4-aminooxy-1-[(2S)-1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL2372132

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Activity

IC50 = 55000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-[(E)-2-methyl-3-phenylprop-2-enylidene]amino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL411819; BDBM50230471

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Activity

IC50 = 58000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-2-[[(2S,4S)-4-[(Z)-benzylideneamino]oxy-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL251891; BDBM50230468

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Activity

IC50 = 64000 nM

[1]

Compound Name

(4S)-4-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S,3R)-2-[[(2S,4R)-1-[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]-4-[(E)-(3,4-dimethoxyphenyl)methylideneamino]oxypyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-4-carboxybutanoyl]amino]-5-amino-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL1946129; BDBM50362889

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Activity

IC50 = 72000 nM

[2]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-3-carboxypropylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL410011; BDBM50230458

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Activity

IC50 = 75000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-3-phenylpropylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL414027; BDBM50230443

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Activity

IC50 = 83000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-(4-nitrophenyl)methylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL403544; BDBM50230489

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Activity

IC50 = 91000 nM

[1]

Compound Name

5-[(Z)-[(3S,5S)-5-[[(2S)-1-[[(2S)-1-Amino-4-carboxy-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]carbamoyl]-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]pyrrolidin-3-yl]oxyiminomethyl]-2-hydroxybenzoic acid

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Investigative

Compound Info

Synonyms

CHEMBL267620; BDBM50230459

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Activity

IC50 = 93000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-(3,4-dimethoxyphenyl)methylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL403545; BDBM50230472

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Activity

IC50 = 114000 nM

[1]

Compound Name

(4S)-5-Amino-4-[[(2S)-4-carboxy-2-[[(2S,4S)-1-[1-[(2S)-2-[[(2S,3R)-2-[[(2S)-1-[(2S)-4-carboxy-2-[[(2S)-1-[5-[(3',6'-dihydroxy-1-oxospiro[2-benzofuran-3,9'-xanthene]-5-yl)carbamothioylamino]pentanoyl]pyrrolidine-2-carbonyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]propanoyl]piperidine-2-carbonyl]-4-[(Z)-(2,3,4,5,6-pentafluorophenyl)methylideneamino]oxypyrrolidine-2-carbonyl]amino]butanoyl]amino]-5-oxopentanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL411342; BDBM50230488

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Activity

IC50 = 139000 nM

[1]

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References

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REF 1

Protected aminooxyprolines for expedited library synthesis: application to Tsg101-directed proline-oxime containing peptides. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1096-101.

REF 2

Elucidation of New Binding Interactions with the Tumor Susceptibility Gene 101 (Tsg101) Protein Using Modified HIV-1 Gag-p6 Derived Peptide Ligands. ACS Med Chem Lett. 2011 May 12;2(5):337-341.

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