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Assay Detail

CHEMBL2051716

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

Binding
Inhibition of N-terminus His6-tagged human kallikrein 6 expressed in baculovirus infected insect sf9 cells using Boc-Phe-Ser-Arg-AMC as substrate by fluorescence analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group.
Liang G, Chen X, Aldous S, Pu SF, Mehdi S, Powers E, Giovanni A, Kongsamut S, Xia T, Zhang Y, Wang R, Gao Z, Merriman G, McLean LR, Morize I.
ACS Med Chem Lett (2012) 3 : 159 -164
PubMed 24900446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.39 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047313 1 5.82
CHEMBL2047314 1 5.54
CHEMBL435585 1 5.11
CHEMBL2047315 1 5.09
CHEMBL331939 1 -
CHEMBL331943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047313 IC50 = 1500.0 nM 5.82
CHEMBL2047314 IC50 = 2900.0 nM 5.54
CHEMBL435585 IC50 = 7750.0 nM 5.11
CHEMBL2047315 IC50 = 8200.0 nM 5.09
CHEMBL331939 IC50 > 30000.0 nM -
CHEMBL331943 IC50 > 30000.0 nM -