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Assay Detail

CHEMBL1693335

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

Functional
Cytotoxicity against human NCI-H146 after 48 hrs by MTS assay in presence of 10% human serum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H146
Confidence 1 — Organism
Curated By Autocuration

Publication

Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
Sleebs BE, Czabotar PE, Fairbrother WJ, Fairlie WD, Flygare JA, Huang DC, Kersten WJ, Koehler MF, Lessene G, Lowes K, Parisot JP, Smith BJ, Smith ML, Souers AJ, Street IP, Yang H, Baell JB.
J Med Chem (2011) 54 : 1914 -1926
PubMed 21366295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.16 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443684 NAVITOCLAX 3.0 1 7.10
CHEMBL1689143 1 6.27
CHEMBL1689139 1 6.21
CHEMBL1689142 1 6.20
CHEMBL1689145 1 6.15
CHEMBL1689146 1 5.96
CHEMBL1689144 1 5.92
CHEMBL1689140 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443684 NAVITOCLAX EC50 = 80.0 nM 7.10
CHEMBL1689143 EC50 = 540.0 nM 6.27
CHEMBL1689139 EC50 = 610.0 nM 6.21
CHEMBL1689142 EC50 = 630.0 nM 6.20
CHEMBL1689145 EC50 = 710.0 nM 6.15
CHEMBL1689146 EC50 = 1100.0 nM 5.96
CHEMBL1689144 EC50 = 1200.0 nM 5.92
CHEMBL1689140 EC50 = 3700.0 nM 5.43