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Assay Detail

CHEMBL4200947

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

Binding
Inhibition of mouse His-tagged IDE (42 to 1019 residues) using fluorophore/quencher-tagged RPPGFSAFK(Dnp)-OH peptide as substrate preincubated for 10 mins followed by substrate addition measured over 5 mins by TR-FRET assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Insulin-degrading enzyme (CHEMBL3232680)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Stabilized β-Hairpin Peptide Inhibits Insulin Degrading Enzyme.
Yang D, Qin W, Shi X, Zhu B, Xie M, Zhao H, Teng B, Wu Y, Zhao R, Yin F, Ren P, Liu L, Li Z.
J Med Chem (2018) 61 : 8174 -8185
PubMed 30148634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.97 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211248 1 7.66
CHEMBL4211765 1 7.36
CHEMBL4206878 1 7.22
CHEMBL4208119 1 7.13
CHEMBL4207403 1 7.11
CHEMBL4203249 1 7.07
CHEMBL4215687 1 6.77
CHEMBL4210721 1 6.64
CHEMBL4216209 1 6.52
CHEMBL4203477 1 6.22
CHEMBL4208342 1 -
CHEMBL4204003 1 -
CHEMBL4202518 1 -
CHEMBL1200558 BACITRACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211248 IC50 = 22.0 nM 7.66
CHEMBL4211765 IC50 = 44.0 nM 7.36
CHEMBL4206878 IC50 = 60.0 nM 7.22
CHEMBL4208119 IC50 = 74.0 nM 7.13
CHEMBL4207403 IC50 = 77.0 nM 7.11
CHEMBL4203249 IC50 = 86.0 nM 7.07
CHEMBL4215687 IC50 = 170.0 nM 6.77
CHEMBL4210721 IC50 = 230.0 nM 6.64
CHEMBL4216209 IC50 = 300.0 nM 6.52
CHEMBL4203477 IC50 = 601.0 nM 6.22
CHEMBL4208342 IC50 > 20000.0 nM -
CHEMBL4204003 IC50 > 20000.0 nM -
CHEMBL4202518 IC50 - -
CHEMBL1200558 BACITRACIN IC50 > 200000.0 nM -