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Assay Detail

CHEMBL898855

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

Binding
Inhibition of human DPP4 in presence of 50 % human serum
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 Intermediate

Target

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

Publication

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL.
Bioorg Med Chem Lett (2007) 17 : 5806 -5811
PubMed 17851076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.60 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237997 1 7.64
CHEMBL400841 1 7.58
CHEMBL237152 1 7.55
CHEMBL235199 1 6.92
CHEMBL437557 1 6.89
CHEMBL238191 1 6.89
CHEMBL237151 1 6.82
CHEMBL238190 1 6.54
CHEMBL392524 1 6.41
CHEMBL235198 1 6.35
CHEMBL237783 1 6.17
CHEMBL237566 1 6.09
CHEMBL237972 1 5.82
CHEMBL235223 1 5.72
CHEMBL235004 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237997 IC50 = 23.0 nM 7.64
CHEMBL400841 IC50 = 26.0 nM 7.58
CHEMBL237152 IC50 = 28.0 nM 7.55
CHEMBL235199 IC50 = 120.0 nM 6.92
CHEMBL437557 IC50 = 130.0 nM 6.89
CHEMBL238191 IC50 = 130.0 nM 6.89
CHEMBL237151 IC50 = 150.0 nM 6.82
CHEMBL238190 IC50 = 290.0 nM 6.54
CHEMBL392524 IC50 = 390.0 nM 6.41
CHEMBL235198 IC50 = 450.0 nM 6.35
CHEMBL237783 IC50 = 670.0 nM 6.17
CHEMBL237566 IC50 = 820.0 nM 6.09
CHEMBL237972 IC50 = 1500.0 nM 5.82
CHEMBL235223 IC50 = 1900.0 nM 5.72
CHEMBL235004 IC50 = 2700.0 nM 5.57