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Assay Detail

CHEMBL4201843

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

Binding
Inhibition of KLK6 (unknown origin) expressed in Pichia pastoris pre-incubated for 10 mins before Boc-ValProArg-AMC substrate addition and measured after 30 mins by fluorescence based assay
2
Total Activities
2
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

Kallikrein-6 (CHEMBL4448)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity.
De Vita E, Schüler P, Lovell S, Lohbeck J, Kullmann S, Rabinovich E, Sananes A, Heßling B, Hamon V, Papo N, Hess J, Tate EW, Gunkel N, Miller AK.
J Med Chem (2018) 61 : 8859 -8874
PubMed 30212625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.99 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206734 1 7.64
CHEMBL4218203 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206734 IC50 = 23.0 nM 7.64
CHEMBL4218203 IC50 = 470.0 nM 6.33