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Assay Detail

CHEMBL4773299

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Binding
Inhibition of recombinant human PTP1B using pNPP as substrate measured after 30 mins
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors.
Lei S,Zhang D,Qi Y,Chowdhury SR,Sun R,Wang J,Du Y,Fu L,Jiang F
Eur J Med Chem (2020) 205 : 112508 -112508
PubMed 32738350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.51 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294467 SODIUM VANADATE 1 7.34
CHEMBL4788887 1 6.46
CHEMBL4786441 1 6.42
CHEMBL4798517 1 6.40
CHEMBL4800140 1 6.39
CHEMBL4788294 1 6.37
CHEMBL4785543 1 6.17
CHEMBL4793462 1 6.12
CHEMBL4787688 1 6.00
CHEMBL4782087 1 5.98
CHEMBL4782460 1 5.57
CHEMBL4781365 1 5.24
CHEMBL4781042 1 4.88
CHEMBL4778849 1 4.75
CHEMBL4777827 1 4.74
CHEMBL4800515 1 4.68
CHEMBL4786486 1 4.66
CHEMBL4776892 1 4.60
CHEMBL4788179 1 4.39
CHEMBL4792019 1 4.29
CHEMBL4780652 1 4.19
CHEMBL4793782 1 -
CHEMBL4796676 1 -
CHEMBL459016 GENIPIN 3.0 1 -
CHEMBL462894 GENIPOSIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294467 SODIUM VANADATE IC50 = 46.0 nM 7.34
CHEMBL4788887 IC50 = 350.0 nM 6.46
CHEMBL4786441 IC50 = 380.0 nM 6.42
CHEMBL4798517 IC50 = 400.0 nM 6.40
CHEMBL4800140 IC50 = 410.0 nM 6.39
CHEMBL4788294 IC50 = 430.0 nM 6.37
CHEMBL4785543 IC50 = 680.0 nM 6.17
CHEMBL4793462 IC50 = 750.0 nM 6.12
CHEMBL4787688 IC50 = 990.0 nM 6.00
CHEMBL4782087 IC50 = 1050.0 nM 5.98
CHEMBL4782460 IC50 = 2670.0 nM 5.57
CHEMBL4781365 IC50 = 5800.0 nM 5.24
CHEMBL4781042 IC50 = 13150.0 nM 4.88
CHEMBL4778849 IC50 = 17690.0 nM 4.75
CHEMBL4777827 IC50 = 18270.0 nM 4.74
CHEMBL4800515 IC50 = 20820.0 nM 4.68
CHEMBL4786486 IC50 = 21740.0 nM 4.66
CHEMBL4776892 IC50 = 25230.0 nM 4.60
CHEMBL4788179 IC50 = 40300.0 nM 4.39
CHEMBL4792019 IC50 = 50760.0 nM 4.29
CHEMBL4780652 IC50 = 64740.0 nM 4.19
CHEMBL4793782 IC50 = 236140.0 nM -
CHEMBL4796676 IC50 > 100000.0 nM -
CHEMBL459016 GENIPIN IC50 > 500000.0 nM -
CHEMBL462894 GENIPOSIDE IC50 > 500000.0 nM -