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Assay Detail

CHEMBL4223222

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

Binding
Inhibition of human cathepsin K
19
Total Activities
19
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

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Nizi E, Sferrazza A, Fabbrini D, Nardi V, Andreini M, Graziani R, Gennari N, Bresciani A, Paonessa G, Harper S.
Bioorg Med Chem Lett (2018) 28 : 1540 -1544
PubMed 29615344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.28 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228926 1 9.96
CHEMBL1215628 1 9.70
CHEMBL4228143 1 9.00
CHEMBL4227295 1 8.89
CHEMBL4228861 1 6.70
CHEMBL4226767 1 6.67
CHEMBL4224829 1 6.36
CHEMBL4228604 1 6.06
CHEMBL4227965 1 5.73
CHEMBL4225367 1 5.57
CHEMBL4225099 1 5.42
CHEMBL4228800 1 -
CHEMBL4227619 1 -
CHEMBL4227566 1 -
CHEMBL4228399 1 -
CHEMBL4228343 1 -
CHEMBL4229174 1 -
CHEMBL4228081 1 -
CHEMBL4228920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228926 IC50 = 0.11 nM 9.96
CHEMBL1215628 IC50 = 0.2 nM 9.70
CHEMBL4228143 IC50 = 1.0 nM 9.00
CHEMBL4227295 IC50 = 1.3 nM 8.89
CHEMBL4228861 IC50 = 202.0 nM 6.70
CHEMBL4226767 IC50 = 213.0 nM 6.67
CHEMBL4224829 IC50 = 435.0 nM 6.36
CHEMBL4228604 IC50 = 867.0 nM 6.06
CHEMBL4227965 IC50 = 1870.0 nM 5.73
CHEMBL4225367 IC50 = 2690.0 nM 5.57
CHEMBL4225099 IC50 = 3828.0 nM 5.42
CHEMBL4228800 IC50 > 5000.0 nM -
CHEMBL4227619 IC50 > 5000.0 nM -
CHEMBL4227566 IC50 - -
CHEMBL4228399 IC50 > 5000.0 nM -
CHEMBL4228343 IC50 > 5000.0 nM -
CHEMBL4229174 IC50 > 5000.0 nM -
CHEMBL4228081 IC50 > 5000.0 nM -
CHEMBL4228920 IC50 > 5000.0 nM -