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Assay Detail

CHEMBL937837

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

Binding
Inhibition of chymotrypsin-like activity of human 20S proteasome
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.
Huang L, Yu D, Ho P, Qian K, Lee KH, Chen CH.
Bioorg Med Chem (2008) 16 : 6696 -6701
PubMed 18562200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.74 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452714 GLYCYRRHETINIC ACID MONOISOPHTHALATE 1 6.66
CHEMBL448708 1 6.54
CHEMBL449799 GLYCYRRHETINIC ACID MONOTEREPHTHALATE 1 6.51
CHEMBL449516 1 6.46
CHEMBL377754 1 6.06
CHEMBL510989 1 5.98
CHEMBL444697 1 5.86
CHEMBL445988 1 5.75
CHEMBL449992 GLYCYRRHETINIC ACID ISOBUTYTATE 1 5.72
CHEMBL448340 1 5.71
CHEMBL503862 1 5.68
CHEMBL451897 1 5.64
CHEMBL499915 CARBENOXOLONE 2.0 1 5.58
CHEMBL448000 1 5.51
CHEMBL318779 1 5.28
CHEMBL374308 LACTACYSTIN 1 5.25
CHEMBL505928 1 5.16
CHEMBL504427 1 5.06
CHEMBL230006 ENOXOLONE 2.0 1 4.65
CHEMBL502680 1 -
CHEMBL450046 GLYCYRRHETINIC ACID PROPIONATE 1 -
CHEMBL207413 ACETOXOLONE -1.0 1 -
CHEMBL510599 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452714 GLYCYRRHETINIC ACID MONOISOPHTHALATE IC50 = 220.0 nM 6.66
CHEMBL448708 IC50 = 290.0 nM 6.54
CHEMBL449799 GLYCYRRHETINIC ACID MONOTEREPHTHALATE IC50 = 310.0 nM 6.51
CHEMBL449516 IC50 = 350.0 nM 6.46
CHEMBL377754 IC50 = 870.0 nM 6.06
CHEMBL510989 IC50 = 1050.0 nM 5.98
CHEMBL444697 IC50 = 1390.0 nM 5.86
CHEMBL445988 IC50 = 1780.0 nM 5.75
CHEMBL449992 GLYCYRRHETINIC ACID ISOBUTYTATE IC50 = 1920.0 nM 5.72
CHEMBL448340 IC50 = 1930.0 nM 5.71
CHEMBL503862 IC50 = 2080.0 nM 5.68
CHEMBL451897 IC50 = 2270.0 nM 5.64
CHEMBL499915 CARBENOXOLONE IC50 = 2630.0 nM 5.58
CHEMBL448000 IC50 = 3090.0 nM 5.51
CHEMBL318779 IC50 = 5250.0 nM 5.28
CHEMBL374308 LACTACYSTIN IC50 = 5600.0 nM 5.25
CHEMBL505928 IC50 = 6860.0 nM 5.16
CHEMBL504427 IC50 = 8700.0 nM 5.06
CHEMBL230006 ENOXOLONE IC50 = 22300.0 nM 4.65
CHEMBL502680 IC50 > 40000.0 nM -
CHEMBL450046 GLYCYRRHETINIC ACID PROPIONATE IC50 > 40000.0 nM -
CHEMBL207413 ACETOXOLONE IC50 > 40000.0 nM -
CHEMBL510599 IC50 > 40000.0 nM -