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Assay Detail

CHEMBL985439

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

Binding
Inhibition of DPP4 in human plasma by fluorescence assay
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 4 (CHEMBL284)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.
Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K.
Bioorg Med Chem (2008) 16 : 4093 -4106
PubMed 18243000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 8.09 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1744354 1 8.96
CHEMBL487860 1 8.82
CHEMBL521224 1 8.62
CHEMBL470477 1 8.59
CHEMBL500008 1 8.57
CHEMBL487680 1 8.55
CHEMBL488036 1 8.54
CHEMBL512726 1 8.54
CHEMBL451937 1 8.51
CHEMBL470476 1 8.51
CHEMBL469659 1 8.51
CHEMBL470681 1 8.48
CHEMBL513725 1 8.48
CHEMBL511785 1 8.39
CHEMBL488418 1 8.35
CHEMBL472096 1 8.34
CHEMBL469660 1 8.28
CHEMBL488419 1 8.27
CHEMBL519585 1 8.24
CHEMBL487861 1 8.24
CHEMBL471088 1 8.21
CHEMBL77538 1 8.15
CHEMBL470893 1 8.14
CHEMBL472102 1 8.11
CHEMBL487681 1 8.09
CHEMBL454193 1 8.08
CHEMBL471089 1 8.07
CHEMBL469452 1 8.06
CHEMBL512890 1 7.92
CHEMBL1203962 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1744354 IC50 = 1.1 nM 8.96
CHEMBL487860 IC50 = 1.5 nM 8.82
CHEMBL521224 IC50 = 2.4 nM 8.62
CHEMBL470477 IC50 = 2.6 nM 8.59
CHEMBL500008 IC50 = 2.7 nM 8.57
CHEMBL487680 IC50 = 2.8 nM 8.55
CHEMBL488036 IC50 = 2.9 nM 8.54
CHEMBL512726 IC50 = 2.9 nM 8.54
CHEMBL451937 IC50 = 3.1 nM 8.51
CHEMBL470476 IC50 = 3.1 nM 8.51
CHEMBL469659 IC50 = 3.1 nM 8.51
CHEMBL513725 IC50 = 3.3 nM 8.48
CHEMBL470681 IC50 = 3.3 nM 8.48
CHEMBL511785 IC50 = 4.1 nM 8.39
CHEMBL488418 IC50 = 4.5 nM 8.35
CHEMBL472096 IC50 = 4.6 nM 8.34
CHEMBL469660 IC50 = 5.3 nM 8.28
CHEMBL488419 IC50 = 5.4 nM 8.27
CHEMBL519585 IC50 = 5.7 nM 8.24
CHEMBL487861 IC50 = 5.8 nM 8.24
CHEMBL471088 IC50 = 6.2 nM 8.21
CHEMBL77538 IC50 = 7.0 nM 8.15
CHEMBL470893 IC50 = 7.3 nM 8.14
CHEMBL472102 IC50 = 7.8 nM 8.11
CHEMBL487681 IC50 = 8.2 nM 8.09
CHEMBL454193 IC50 = 8.3 nM 8.08
CHEMBL471089 IC50 = 8.6 nM 8.07
CHEMBL469452 IC50 = 8.7 nM 8.06
CHEMBL512890 IC50 = 12.0 nM 7.92
CHEMBL1203962 IC50 = 13.0 nM 7.89
CHEMBL487862 IC50 = 13.0 nM 7.89
CHEMBL508845 IC50 = 16.0 nM 7.80
CHEMBL512694 IC50 = 22.0 nM 7.66
CHEMBL472101 IC50 = 27.0 nM 7.57
CHEMBL520854 IC50 = 31.0 nM 7.51
CHEMBL470330 IC50 = 33.0 nM 7.48
CHEMBL485828 IC50 = 39.0 nM 7.41
CHEMBL485827 IC50 = 75.0 nM 7.12
CHEMBL472100 IC50 = 88.0 nM 7.06
CHEMBL488810 IC50 = 109.0 nM 6.96
CHEMBL511128 IC50 = 252.0 nM 6.60
CHEMBL504237 IC50 > 316.0 nM -
CHEMBL472097 IC50 > 316.0 nM -