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Assay Detail

CHEMBL3620563

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to FAP (unknown origin)
35
Total Activities
35
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

Prolyl endopeptidase FAP (CHEMBL4683)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold
Jansen K, De Winter H, Heirbaut L, Cheng JD, Joossens J, Lambeir A, De Meester I, Augustyns K, Van der Veken P
Medchemcomm (2014) 5 : 1700 -1707
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.89 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233842 1 8.48
CHEMBL67279 TALABOSTAT 3.0 1 7.16
CHEMBL237500 LINAGLIPTIN 4.0 1 6.43
CHEMBL3616890 1 6.13
CHEMBL3616901 1 5.92
CHEMBL3616900 1 5.75
CHEMBL3616895 1 5.72
CHEMBL3616896 1 5.48
CHEMBL3616917 1 5.24
CHEMBL3616902 1 4.99
CHEMBL3616891 1 4.96
CHEMBL3616903 1 4.39
CHEMBL3616892 1 -
CHEMBL3616888 1 -
CHEMBL3616904 1 -
CHEMBL3616905 1 -
CHEMBL3616906 1 -
CHEMBL3616907 1 -
CHEMBL3616908 1 -
CHEMBL3616919 1 -
CHEMBL3616918 1 -
CHEMBL3616916 1 -
CHEMBL3616915 1 -
CHEMBL3616914 1 -
CHEMBL3616913 1 -
CHEMBL3616909 1 -
CHEMBL3616920 1 -
CHEMBL3616910 1 -
CHEMBL3616912 1 -
CHEMBL3616911 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233842 IC50 = 3.3 nM 8.48
CHEMBL67279 TALABOSTAT IC50 = 70.0 nM 7.16
CHEMBL237500 LINAGLIPTIN IC50 = 370.0 nM 6.43
CHEMBL3616890 IC50 = 740.0 nM 6.13
CHEMBL3616901 IC50 = 1200.0 nM 5.92
CHEMBL3616900 IC50 = 1800.0 nM 5.75
CHEMBL3616895 IC50 = 1900.0 nM 5.72
CHEMBL3616896 IC50 = 3300.0 nM 5.48
CHEMBL3616917 IC50 = 5800.0 nM 5.24
CHEMBL3616902 IC50 = 10300.0 nM 4.99
CHEMBL3616891 IC50 = 11000.0 nM 4.96
CHEMBL3616903 IC50 = 41000.0 nM 4.39
CHEMBL3616899 IC50 > 10000.0 nM -
CHEMBL3616898 IC50 > 10000.0 nM -
CHEMBL3616897 IC50 > 100000.0 nM -
CHEMBL3616894 IC50 > 10000.0 nM -
CHEMBL3616893 IC50 > 100000.0 nM -
CHEMBL3616892 IC50 > 10000.0 nM -
CHEMBL3616888 IC50 > 100000.0 nM -
CHEMBL3616904 IC50 > 100000.0 nM -
CHEMBL3616905 IC50 > 100000.0 nM -
CHEMBL3616906 IC50 > 100000.0 nM -
CHEMBL3616907 IC50 > 100000.0 nM -
CHEMBL3616908 IC50 > 50000.0 nM -
CHEMBL3616919 IC50 > 50000.0 nM -
CHEMBL3616918 IC50 - -
CHEMBL3616916 IC50 > 100000.0 nM -
CHEMBL3616915 IC50 > 100000.0 nM -
CHEMBL3616914 IC50 > 100000.0 nM -
CHEMBL3616913 IC50 > 100000.0 nM -
CHEMBL3616909 IC50 > 100000.0 nM -
CHEMBL3616920 IC50 - -
CHEMBL3616910 IC50 > 12500.0 nM -
CHEMBL3616912 IC50 > 100000.0 nM -
CHEMBL3616911 IC50 > 100000.0 nM -