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Assay Detail

CHEMBL832699

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

Binding
Inhibitory concentration against rat dipeptidylpeptidase IV
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dipeptidyl peptidase 4 (CHEMBL4653)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
Sakashita H, Kitajima H, Nakamura M, Akahoshi F, Hayashi Y.
Bioorg Med Chem Lett (2005) 15 : 2441 -2445
PubMed 15863294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 9.00 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194717 1 9.82
CHEMBL370540 1 9.77
CHEMBL370046 1 9.77
CHEMBL433811 1 9.62
CHEMBL371143 1 9.59
CHEMBL195420 1 9.57
CHEMBL195063 1 9.55
CHEMBL195335 1 9.28
CHEMBL371585 1 8.96
CHEMBL194993 1 8.82
CHEMBL77538 1 8.64
CHEMBL381626 1 8.54
CHEMBL195804 1 8.52
CHEMBL192882 1 8.44
CHEMBL539939 1 8.42
CHEMBL193168 1 8.41
CHEMBL192165 1 8.17
CHEMBL191699 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194717 IC50 = 0.15 nM 9.82
CHEMBL370540 IC50 = 0.17 nM 9.77
CHEMBL370046 IC50 = 0.17 nM 9.77
CHEMBL433811 IC50 = 0.24 nM 9.62
CHEMBL371143 IC50 = 0.26 nM 9.59
CHEMBL195420 IC50 = 0.27 nM 9.57
CHEMBL195063 IC50 = 0.28 nM 9.55
CHEMBL195335 IC50 = 0.53 nM 9.28
CHEMBL371585 IC50 = 1.1 nM 8.96
CHEMBL194993 IC50 = 1.5 nM 8.82
CHEMBL77538 IC50 = 2.3 nM 8.64
CHEMBL381626 IC50 = 2.9 nM 8.54
CHEMBL195804 IC50 = 3.0 nM 8.52
CHEMBL192882 IC50 = 3.6 nM 8.44
CHEMBL539939 IC50 = 3.8 nM 8.42
CHEMBL193168 IC50 = 3.9 nM 8.41
CHEMBL192165 IC50 = 6.7 nM 8.17
CHEMBL191699 IC50 = 9.1 nM 8.04