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Assay Detail

CHEMBL988354

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

Binding
Inhibition of DPP2
41
Total Activities
41
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.
Sattigeri JA, Andappan MM, Kishore K, Thangathirupathy S, Sundaram S, Singh S, Sharma S, Davis JA, Chugh A, Bansal VS.
Bioorg Med Chem Lett (2008) 18 : 4087 -4091
PubMed 18602260 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.53 7.02
Activity 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479538 1 7.02
CHEMBL93505 1 6.79
CHEMBL482104 1 6.65
CHEMBL471960 1 6.39
CHEMBL481290 1 6.04
CHEMBL481669 1 6.00
CHEMBL481288 1 6.00
CHEMBL479567 1 5.92
CHEMBL520266 1 5.89
CHEMBL481177 1 5.89
CHEMBL452998 1 5.87
CHEMBL480942 1 5.75
CHEMBL482262 1 5.66
CHEMBL479381 1 5.56
CHEMBL480712 1 5.55
CHEMBL520921 1 5.41
CHEMBL480324 1 5.40
CHEMBL480781 1 5.36
CHEMBL480536 1 5.29
CHEMBL480537 1 5.29
CHEMBL480705 1 5.19
CHEMBL471956 1 5.06
CHEMBL480914 1 5.05
CHEMBL480154 1 5.00
CHEMBL511125 1 4.97
CHEMBL479983 1 4.96
CHEMBL520434 1 4.96
CHEMBL519265 1 4.96
CHEMBL479736 1 4.88
CHEMBL482261 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479538 IC50 = 96.0 nM 7.02
CHEMBL93505 IC50 = 163.0 nM 6.79
CHEMBL482104 IC50 = 226.0 nM 6.65
CHEMBL471960 IC50 = 406.0 nM 6.39
CHEMBL481290 IC50 = 907.0 nM 6.04
CHEMBL481669 IC50 = 1000.0 nM 6.00
CHEMBL481288 IC50 = 1000.0 nM 6.00
CHEMBL479567 IC50 = 1200.0 nM 5.92
CHEMBL520266 IC50 = 1300.0 nM 5.89
CHEMBL481177 IC50 = 1300.0 nM 5.89
CHEMBL452998 IC50 = 1340.0 nM 5.87
CHEMBL480942 IC50 = 1800.0 nM 5.75
CHEMBL482262 IC50 = 2200.0 nM 5.66
CHEMBL479381 IC50 = 2760.0 nM 5.56
CHEMBL480712 IC50 = 2800.0 nM 5.55
CHEMBL520921 IC50 = 3900.0 nM 5.41
CHEMBL480324 IC50 = 4000.0 nM 5.40
CHEMBL480781 IC50 = 4330.0 nM 5.36
CHEMBL480536 IC50 = 5100.0 nM 5.29
CHEMBL480537 IC50 = 5100.0 nM 5.29
CHEMBL480705 IC50 = 6420.0 nM 5.19
CHEMBL471956 IC50 = 8750.0 nM 5.06
CHEMBL480914 IC50 = 9000.0 nM 5.05
CHEMBL480154 IC50 = 9880.0 nM 5.00
CHEMBL511125 IC50 = 10800.0 nM 4.97
CHEMBL479983 IC50 = 11000.0 nM 4.96
CHEMBL520434 IC50 = 10900.0 nM 4.96
CHEMBL519265 IC50 = 11000.0 nM 4.96
CHEMBL479736 IC50 = 13050.0 nM 4.88
CHEMBL482261 IC50 = 16500.0 nM 4.78
CHEMBL479380 IC50 = 18100.0 nM 4.74
CHEMBL480155 IC50 = 21800.0 nM 4.66
CHEMBL471785 Activity - -
CHEMBL471784 Activity - -
CHEMBL479794 IC50 > 10000.0 nM -
CHEMBL479803 IC50 > 10000.0 nM -
CHEMBL480913 Activity - -
CHEMBL480943 Activity - -
CHEMBL519272 Activity - -
CHEMBL509391 Activity - -
CHEMBL480713 Activity - -