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Assay Detail

CHEMBL933102

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

Binding
Inhibition of bovine alpha chymotrypsin
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Dorsey BD, Iqbal M, Chatterjee S, Menta E, Bernardini R, Bernareggi A, Cassarà PG, D'Arasmo G, Ferretti E, De Munari S, Oliva A, Pezzoni G, Allievi C, Strepponi I, Ruggeri B, Ator MA, Williams M, Mallamo JP.
J Med Chem (2008) 51 : 1068 -1072
PubMed 18247547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.26 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269875 1 6.57
CHEMBL259675 1 6.55
CHEMBL410111 1 6.54
CHEMBL259677 1 6.34
CHEMBL270762 1 6.30
CHEMBL325041 BORTEZOMIB 3.0 1 6.30
CHEMBL272880 1 6.23
CHEMBL407947 1 6.22
CHEMBL270727 1 6.05
CHEMBL270936 1 5.89
CHEMBL270515 DELANZOMIB 2.0 1 5.82
CHEMBL272906 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269875 IC50 = 270.0 nM 6.57
CHEMBL259675 IC50 = 280.0 nM 6.55
CHEMBL410111 IC50 = 290.0 nM 6.54
CHEMBL259677 IC50 = 460.0 nM 6.34
CHEMBL270762 IC50 = 500.0 nM 6.30
CHEMBL325041 BORTEZOMIB IC50 = 500.0 nM 6.30
CHEMBL272880 IC50 = 590.0 nM 6.23
CHEMBL407947 IC50 = 600.0 nM 6.22
CHEMBL270727 IC50 = 900.0 nM 6.05
CHEMBL270936 IC50 = 1300.0 nM 5.89
CHEMBL270515 DELANZOMIB IC50 = 1500.0 nM 5.82
CHEMBL272906 IC50 - -