Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3118377

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

Binding
Inhibition of human recombinant DPP4 (39 to 766)
16
Total Activities
16
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

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

Publication

Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.
Namoto K, Sirockin F, Ostermann N, Gessier F, Flohr S, Sedrani R, Gerhartz B, Trappe J, Hassiepen U, Duttaroy A, Ferreira S, Sutton JM, Clark DE, Fenton G, Beswick M, Baeschlin DK.
Bioorg Med Chem Lett (2014) 24 : 731 -736
PubMed 24439847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.85 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3112968 1 8.70
CHEMBL3112959 1 8.52
CHEMBL3112960 1 8.40
CHEMBL3112967 1 8.15
CHEMBL3112971 1 8.05
CHEMBL1422 SITAGLIPTIN 4.0 1 8.00
CHEMBL3112966 1 7.70
CHEMBL3112958 1 7.40
CHEMBL3112970 1 7.40
CHEMBL3112957 1 6.70
CHEMBL3112969 1 6.60
CHEMBL3112964 1 5.38
CHEMBL3112961 1 4.92
CHEMBL3112965 1 4.80
CHEMBL3112962 1 4.70
CHEMBL3112963 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3112968 IC50 = 2.0 nM 8.70
CHEMBL3112959 IC50 = 3.0 nM 8.52
CHEMBL3112960 IC50 = 4.0 nM 8.40
CHEMBL3112967 IC50 = 7.0 nM 8.15
CHEMBL3112971 IC50 = 9.0 nM 8.05
CHEMBL1422 SITAGLIPTIN IC50 = 10.0 nM 8.00
CHEMBL3112966 IC50 = 20.0 nM 7.70
CHEMBL3112958 IC50 = 40.0 nM 7.40
CHEMBL3112970 IC50 = 40.0 nM 7.40
CHEMBL3112957 IC50 = 200.0 nM 6.70
CHEMBL3112969 IC50 = 250.0 nM 6.60
CHEMBL3112964 IC50 = 4200.0 nM 5.38
CHEMBL3112961 IC50 = 11900.0 nM 4.92
CHEMBL3112965 IC50 = 15700.0 nM 4.80
CHEMBL3112962 IC50 = 19900.0 nM 4.70
CHEMBL3112963 IC50 = 60000.0 nM 4.22