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Assay Detail

CHEMBL880568

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Binding
Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Dipeptidyl peptidase 2 (CHEMBL3976)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Hu Y, Ma L, Wu M, Wong MS, Li B, Corral S, Yu Z, Nomanbhoy T, Alemayehu S, Fuller SR, Rosenblum JS, Rozenkrants N, Minimo LC, Ripka WC, Szardenings AK, Kozarich JW, Shreder KR.
Bioorg Med Chem Lett (2005) 15 : 4239 -4242
PubMed 16085416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.59 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372180 1 9.00
CHEMBL196933 1 8.74
CHEMBL196267 1 8.66
CHEMBL382974 1 8.40
CHEMBL371130 1 8.39
CHEMBL196120 1 8.20
CHEMBL362922 1 8.10
CHEMBL371429 1 7.82
CHEMBL381444 1 7.46
CHEMBL305170 1 7.42
CHEMBL427012 1 6.92
CHEMBL382980 1 6.85
CHEMBL373269 1 6.38
CHEMBL381200 1 6.24
CHEMBL196188 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372180 IC50 = 1.0 nM 9.00
CHEMBL196933 IC50 = 1.8 nM 8.74
CHEMBL196267 IC50 = 2.2 nM 8.66
CHEMBL382974 IC50 = 4.0 nM 8.40
CHEMBL371130 IC50 = 4.1 nM 8.39
CHEMBL196120 IC50 = 6.3 nM 8.20
CHEMBL362922 IC50 = 8.0 nM 8.10
CHEMBL371429 IC50 = 15.0 nM 7.82
CHEMBL381444 IC50 = 35.0 nM 7.46
CHEMBL305170 IC50 = 38.0 nM 7.42
CHEMBL427012 IC50 = 120.0 nM 6.92
CHEMBL382980 IC50 = 140.0 nM 6.85
CHEMBL373269 IC50 = 420.0 nM 6.38
CHEMBL381200 IC50 = 570.0 nM 6.24
CHEMBL196188 IC50 = 4600.0 nM 5.34