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Assay Detail

CHEMBL2214126

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

Functional
Antiproliferative activity at human A549 cells after 72 hrs by MTT assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
Lovejoy DB, Sharp DM, Seebacher N, Obeidy P, Prichard T, Stefani C, Basha MT, Sharpe PC, Jansson PJ, Kalinowski DS, Bernhardt PV, Richardson DR.
J Med Chem (2012) 55 : 7230 -7244
PubMed 22861499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.34 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203738 1 9.00
CHEMBL2203739 1 8.40
CHEMBL2203744 1 8.40
CHEMBL2203740 1 8.00
CHEMBL888 GEMCITABINE 4.0 1 7.70
CHEMBL385064 1 7.70
CHEMBL44657 ETOPOSIDE 4.0 1 6.10
CHEMBL390195 1 5.66
CHEMBL556 DEFEROXAMINE 4.0 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203738 IC50 = 1.0 nM 9.00
CHEMBL2203739 IC50 = 4.0 nM 8.40
CHEMBL2203744 IC50 = 4.0 nM 8.40
CHEMBL2203740 IC50 = 10.0 nM 8.00
CHEMBL888 GEMCITABINE IC50 = 20.0 nM 7.70
CHEMBL385064 IC50 = 20.0 nM 7.70
CHEMBL44657 ETOPOSIDE IC50 = 800.0 nM 6.10
CHEMBL390195 IC50 = 2200.0 nM 5.66
CHEMBL556 DEFEROXAMINE IC50 = 7500.0 nM 5.12