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Assay Detail

CHEMBL665783

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Binding
In vitro for inhibition of Dipeptidylpeptidase IV.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.
Coutts SJ, Kelly TA, Snow RJ, Kennedy CA, Barton RW, Adams J, Krolikowski DA, Freeman DM, Campbell SJ, Ksiazek JF, Bachovchin WW.
J Med Chem (1996) 39 : 2087 -2094
PubMed 8642568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.76 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66032 1 7.96
CHEMBL63860 1 7.82
CHEMBL63895 1 7.70
CHEMBL1790483 1 7.60
CHEMBL67279 TALABOSTAT 3.0 1 7.58
CHEMBL304007 1 7.50
CHEMBL63698 1 7.36
CHEMBL63406 1 7.22
CHEMBL291428 1 7.20
CHEMBL63652 1 7.16
CHEMBL63726 1 7.02
CHEMBL1790478 1 6.72
CHEMBL292342 1 6.60
CHEMBL65406 1 5.40
CHEMBL67089 1 4.80
CHEMBL303131 1 4.77
CHEMBL66189 1 4.52
CHEMBL305170 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66032 IC50 = 11.0 nM 7.96
CHEMBL63860 IC50 = 15.0 nM 7.82
CHEMBL63895 IC50 = 20.0 nM 7.70
CHEMBL1790483 IC50 = 25.0 nM 7.60
CHEMBL67279 TALABOSTAT IC50 = 26.0 nM 7.58
CHEMBL304007 IC50 = 32.0 nM 7.50
CHEMBL63698 IC50 = 44.0 nM 7.36
CHEMBL63406 IC50 = 60.0 nM 7.22
CHEMBL291428 IC50 = 63.0 nM 7.20
CHEMBL63652 IC50 = 70.0 nM 7.16
CHEMBL63726 IC50 = 95.0 nM 7.02
CHEMBL1790478 IC50 = 190.0 nM 6.72
CHEMBL292342 IC50 = 250.0 nM 6.60
CHEMBL65406 IC50 = 4000.0 nM 5.40
CHEMBL67089 IC50 = 16000.0 nM 4.80
CHEMBL303131 IC50 = 17000.0 nM 4.77
CHEMBL66189 IC50 = 30000.0 nM 4.52
CHEMBL305170 IC50 = 116000.0 nM -