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Assay Detail

CHEMBL4267486

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Binding
Inhibition of human tPA
9
Total Activities
9
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

Tissue-type plasminogen activator (CHEMBL1873)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of selective urokinase plasminogen activator (uPA) inhibitors as a potential treatment for multiple sclerosis.
Islam I, Yuan S, West CW, Adler M, Bothe U, Bryant J, Chang Z, Chu K, Emayan K, Gualtieri G, Ho E, Light D, Mallari C, Morser J, Phillips G, Schaefer C, Sukovich D, Whitlow M, Chen D, Buckman BO.
Bioorg Med Chem Lett (2018) 28 : 3372 -3375
PubMed 30201291 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.79 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281179 1 6.33
CHEMBL4281574 1 5.84
CHEMBL4277939 1 5.80
CHEMBL4285028 1 5.80
CHEMBL4291446 1 5.73
CHEMBL4288828 1 5.24
CHEMBL4278454 1 -
CHEMBL4277252 1 -
CHEMBL4290603 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281179 IC50 = 470.0 nM 6.33
CHEMBL4281574 IC50 = 1450.0 nM 5.84
CHEMBL4277939 IC50 = 1600.0 nM 5.80
CHEMBL4285028 IC50 = 1580.0 nM 5.80
CHEMBL4291446 IC50 = 1850.0 nM 5.73
CHEMBL4288828 IC50 = 5700.0 nM 5.24
CHEMBL4278454 IC50 - -
CHEMBL4277252 IC50 - -
CHEMBL4290603 IC50 > 30000.0 nM -