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Assay Detail

CHEMBL3737792

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Binding
Inhibition of bovine serum FAP
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase FAP (CHEMBL3734641)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T.
Bioorg Med Chem Lett (2015) 25 : 5767 -5771
PubMed 26546218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 4.57 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3734999 1 5.42
CHEMBL3736137 1 5.20
CHEMBL3734769 1 5.06
CHEMBL3735843 1 4.85
CHEMBL3735694 1 4.80
CHEMBL3735917 1 4.70
CHEMBL3734964 1 4.66
CHEMBL3645492 1 4.58
CHEMBL3735925 1 4.57
CHEMBL3734828 1 4.50
CHEMBL3735461 1 4.50
CHEMBL3735129 1 4.40
CHEMBL3735852 1 4.35
CHEMBL3736135 1 4.33
CHEMBL3736085 1 4.30
CHEMBL3736190 1 4.27
CHEMBL3735433 1 4.22
CHEMBL3735281 1 4.16
CHEMBL3736423 1 4.02
CHEMBL3736067 1 -
CHEMBL2425070 1 -
CHEMBL3736511 1 -
CHEMBL3735329 1 -
CHEMBL3735865 1 -
CHEMBL3734912 1 -
CHEMBL3736188 1 -
CHEMBL2105762 OMARIGLIPTIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3734999 IC50 = 3800.0 nM 5.42
CHEMBL3736137 IC50 = 6300.0 nM 5.20
CHEMBL3734769 IC50 = 8800.0 nM 5.06
CHEMBL3735843 IC50 = 14000.0 nM 4.85
CHEMBL3735694 IC50 = 16000.0 nM 4.80
CHEMBL3735917 IC50 = 20000.0 nM 4.70
CHEMBL3734964 IC50 = 22000.0 nM 4.66
CHEMBL3645492 IC50 = 26000.0 nM 4.58
CHEMBL3735925 IC50 = 27000.0 nM 4.57
CHEMBL3734828 IC50 = 32000.0 nM 4.50
CHEMBL3735461 IC50 = 32000.0 nM 4.50
CHEMBL3735129 IC50 = 40000.0 nM 4.40
CHEMBL3735852 IC50 = 45000.0 nM 4.35
CHEMBL3736135 IC50 = 47000.0 nM 4.33
CHEMBL3736085 IC50 = 50000.0 nM 4.30
CHEMBL3736190 IC50 = 54000.0 nM 4.27
CHEMBL3735433 IC50 = 60000.0 nM 4.22
CHEMBL3735281 IC50 = 69000.0 nM 4.16
CHEMBL3736423 IC50 = 95000.0 nM 4.02
CHEMBL3736067 IC50 > 100000.0 nM -
CHEMBL2425070 IC50 > 100000.0 nM -
CHEMBL3736511 IC50 > 100000.0 nM -
CHEMBL3735329 IC50 > 100000.0 nM -
CHEMBL3735865 IC50 > 100000.0 nM -
CHEMBL3734912 IC50 > 100000.0 nM -
CHEMBL3736188 IC50 > 100000.0 nM -
CHEMBL2105762 OMARIGLIPTIN IC50 > 100000.0 nM -