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Assay Detail

CHEMBL1764645

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Binding
Inhibition of chymotrypsin-like activity of 20S proteasome
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and proteasome inhibition of lithocholic acid derivatives.
Dang Z, Lin A, Ho P, Soroka D, Lee KH, Huang L, Chen CH.
Bioorg Med Chem Lett (2011) 21 : 1926 -1928
PubMed 21388808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.21 5.72
Inhibition 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1760879 1 5.72
CHEMBL1760876 1 5.66
CHEMBL1760873 1 5.46
CHEMBL1760880 1 5.42
CHEMBL318779 1 5.28
CHEMBL374308 LACTACYSTIN 1 5.25
CHEMBL1760871 1 5.24
CHEMBL1760875 1 5.16
CHEMBL1760877 1 5.07
CHEMBL1760878 1 5.07
CHEMBL1760869 1 4.99
CHEMBL1760872 1 4.97
CHEMBL1760870 1 4.94
CHEMBL1478 LITHOCHOLIC ACID 1 4.74
CHEMBL1760874 1 -
CHEMBL1760868 1 -
CHEMBL1760881 1 -
CHEMBL1760882 1 -
CHEMBL1760883 1 -
CHEMBL260735 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1760879 IC50 = 1900.0 nM 5.72
CHEMBL1760876 IC50 = 2200.0 nM 5.66
CHEMBL1760873 IC50 = 3500.0 nM 5.46
CHEMBL1760880 IC50 = 3800.0 nM 5.42
CHEMBL318779 IC50 = 5200.0 nM 5.28
CHEMBL374308 LACTACYSTIN IC50 = 5600.0 nM 5.25
CHEMBL1760871 IC50 = 5800.0 nM 5.24
CHEMBL1760875 IC50 = 6900.0 nM 5.16
CHEMBL1760877 IC50 = 8500.0 nM 5.07
CHEMBL1760878 IC50 = 8600.0 nM 5.07
CHEMBL1760869 IC50 = 10300.0 nM 4.99
CHEMBL1760872 IC50 = 10800.0 nM 4.97
CHEMBL1760870 IC50 = 11500.0 nM 4.94
CHEMBL1478 LITHOCHOLIC ACID IC50 = 18100.0 nM 4.74
CHEMBL1760874 Inhibition - % -
CHEMBL1760868 Inhibition - % -
CHEMBL1760881 Inhibition - % -
CHEMBL1760882 Inhibition - % -
CHEMBL1760883 Inhibition - % -
CHEMBL260735 Inhibition - % -