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Assay Detail

CHEMBL657293

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

Binding
Inhibition of human cathepsin B
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.
Yasuma T, Oi S, Choh N, Nomura T, Furuyama N, Nishimura A, Fujisawa Y, Sohda T.
J Med Chem (1998) 41 : 4301 -4308
PubMed 9784105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.59 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191881 LEUPEPTIN 1 8.03
CHEMBL374508 E-64 1 7.80
CHEMBL1791004 1 7.64
CHEMBL136252 1 7.52
CHEMBL1790996 1 7.28
CHEMBL132595 1 7.19
CHEMBL134494 1 7.00
CHEMBL1790999 1 6.96
CHEMBL341197 1 6.92
CHEMBL1790991 1 6.66
CHEMBL1790997 1 6.57
CHEMBL1790990 1 6.57
CHEMBL1790994 1 6.51
CHEMBL1790989 1 6.43
CHEMBL1790995 1 6.39
CHEMBL1791000 1 6.36
CHEMBL1791001 1 6.34
CHEMBL334443 1 6.32
CHEMBL342189 1 6.28
CHEMBL1790998 1 6.28
CHEMBL1790992 1 6.24
CHEMBL335942 1 6.11
CHEMBL336415 1 5.89
CHEMBL336591 1 5.85
CHEMBL1790993 1 5.82
CHEMBL135471 1 5.50
CHEMBL334405 1 5.41
CHEMBL134565 1 -
CHEMBL341577 1 -
CHEMBL132652 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191881 LEUPEPTIN IC50 = 9.4 nM 8.03
CHEMBL374508 E-64 IC50 = 16.0 nM 7.80
CHEMBL1791004 IC50 = 23.0 nM 7.64
CHEMBL136252 IC50 = 30.0 nM 7.52
CHEMBL1790996 IC50 = 52.0 nM 7.28
CHEMBL132595 IC50 = 65.0 nM 7.19
CHEMBL134494 IC50 = 100.0 nM 7.00
CHEMBL1790999 IC50 = 110.0 nM 6.96
CHEMBL341197 IC50 = 120.0 nM 6.92
CHEMBL1790991 IC50 = 220.0 nM 6.66
CHEMBL1790997 IC50 = 270.0 nM 6.57
CHEMBL1790990 IC50 = 270.0 nM 6.57
CHEMBL1790994 IC50 = 310.0 nM 6.51
CHEMBL1790989 IC50 = 370.0 nM 6.43
CHEMBL1790995 IC50 = 410.0 nM 6.39
CHEMBL1791000 IC50 = 440.0 nM 6.36
CHEMBL1791001 IC50 = 460.0 nM 6.34
CHEMBL334443 IC50 = 480.0 nM 6.32
CHEMBL342189 IC50 = 530.0 nM 6.28
CHEMBL1790998 IC50 = 530.0 nM 6.28
CHEMBL1790992 IC50 = 580.0 nM 6.24
CHEMBL335942 IC50 = 780.0 nM 6.11
CHEMBL336415 IC50 = 1300.0 nM 5.89
CHEMBL336591 IC50 = 1400.0 nM 5.85
CHEMBL1790993 IC50 = 1500.0 nM 5.82
CHEMBL135471 IC50 = 3200.0 nM 5.50
CHEMBL334405 IC50 = 3900.0 nM 5.41
CHEMBL134565 IC50 > 1000.0 nM -
CHEMBL341577 IC50 > 1000.0 nM -
CHEMBL132652 IC50 > 1000.0 nM -
CHEMBL336748 IC50 > 1000.0 nM -
CHEMBL136024 IC50 > 1000.0 nM -
CHEMBL335007 IC50 > 1000.0 nM -