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Assay Detail

CHEMBL714770

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

Functional
Inhibitory concentration against MOLT-4 cells (human T-cell leukemia cell line)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MOLT-4
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Calpain-1 catalytic subunit (CHEMBL3891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,2-Benzothiazine 1,1-dioxide P(2)-P(3) peptide mimetic aldehyde calpain I inhibitors.
Wells GJ, Tao M, Josef KA, Bihovsky R.
J Med Chem (2001) 44 : 3488 -3503
PubMed 11585453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.72 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269384 1 6.30
CHEMBL326161 1 6.05
CHEMBL118688 1 5.89
CHEMBL420698 1 5.77
CHEMBL333622 1 5.75
CHEMBL332683 1 5.72
CHEMBL115954 1 5.70
CHEMBL269333 1 5.68
CHEMBL331649 1 5.66
CHEMBL117553 1 5.66
CHEMBL331414 1 5.62
CHEMBL115573 1 5.58
CHEMBL421043 1 5.54
CHEMBL117694 1 5.50
CHEMBL117006 1 5.39
CHEMBL115572 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269384 IC50 = 500.0 nM 6.30
CHEMBL326161 IC50 = 900.0 nM 6.05
CHEMBL118688 IC50 = 1300.0 nM 5.89
CHEMBL420698 IC50 = 1700.0 nM 5.77
CHEMBL333622 IC50 = 1800.0 nM 5.75
CHEMBL332683 IC50 = 1900.0 nM 5.72
CHEMBL115954 IC50 = 2000.0 nM 5.70
CHEMBL269333 IC50 = 2100.0 nM 5.68
CHEMBL331649 IC50 = 2200.0 nM 5.66
CHEMBL117553 IC50 = 2200.0 nM 5.66
CHEMBL331414 IC50 = 2400.0 nM 5.62
CHEMBL115573 IC50 = 2600.0 nM 5.58
CHEMBL421043 IC50 = 2900.0 nM 5.54
CHEMBL117694 IC50 = 3200.0 nM 5.50
CHEMBL117006 IC50 = 4100.0 nM 5.39
CHEMBL115572 IC50 > 3000.0 nM -