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Assay Detail

CHEMBL833776

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

Functional
Concentration required for 50% growth inhibition of human A549 cancer cell lines after 3 days of culture
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
Van Quaquebeke E, Simon G, André A, Dewelle J, El Yazidi M, Bruyneel F, Tuti J, Nacoulma O, Guissou P, Decaestecker C, Braekman JC, Kiss R, Darro F.
J Med Chem (2005) 48 : 849 -856
PubMed 15689169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.97 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176316 1 8.70
CHEMBL175946 1 8.52
CHEMBL433564 1 8.40
CHEMBL175947 1 8.40
CHEMBL175452 1 8.40
CHEMBL360322 1 8.30
CHEMBL178993 1 8.10
CHEMBL369587 1 8.05
CHEMBL177836 1 7.75
CHEMBL175806 1 7.60
CHEMBL180496 1 7.38
CHEMBL175716 1 7.32
CHEMBL368047 1 7.13
CHEMBL369515 1 6.90
CHEMBL175719 1 6.38
CHEMBL175769 1 6.33
CHEMBL175921 1 6.20
CHEMBL434923 1 6.18
CHEMBL360496 1 5.73
CHEMBL366906 1 5.59
CHEMBL178933 1 5.57
CHEMBL366970 1 5.44
CHEMBL175981 1 5.43
CHEMBL367124 1 5.33
CHEMBL427124 1 5.12
CHEMBL426228 1 -
CHEMBL262795 1 -
CHEMBL360685 1 -
CHEMBL367694 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176316 IC50 = 2.0 nM 8.70
CHEMBL175946 IC50 = 3.0 nM 8.52
CHEMBL433564 IC50 = 4.0 nM 8.40
CHEMBL175947 IC50 = 4.0 nM 8.40
CHEMBL175452 IC50 = 4.0 nM 8.40
CHEMBL360322 IC50 = 5.0 nM 8.30
CHEMBL178993 IC50 = 8.0 nM 8.10
CHEMBL369587 IC50 = 9.0 nM 8.05
CHEMBL177836 IC50 = 18.0 nM 7.75
CHEMBL175806 IC50 = 25.0 nM 7.60
CHEMBL180496 IC50 = 42.0 nM 7.38
CHEMBL175716 IC50 = 48.0 nM 7.32
CHEMBL368047 IC50 = 74.0 nM 7.13
CHEMBL369515 IC50 = 126.0 nM 6.90
CHEMBL175719 IC50 = 414.0 nM 6.38
CHEMBL175769 IC50 = 463.0 nM 6.33
CHEMBL175921 IC50 = 625.0 nM 6.20
CHEMBL434923 IC50 = 657.0 nM 6.18
CHEMBL360496 IC50 = 1861.0 nM 5.73
CHEMBL366906 IC50 = 2580.0 nM 5.59
CHEMBL178933 IC50 = 2720.0 nM 5.57
CHEMBL366970 IC50 = 3652.0 nM 5.44
CHEMBL175981 IC50 = 3705.0 nM 5.43
CHEMBL367124 IC50 = 4731.0 nM 5.33
CHEMBL427124 IC50 = 7544.0 nM 5.12
CHEMBL426228 IC50 > 10000.0 nM -
CHEMBL262795 IC50 > 10000.0 nM -
CHEMBL360685 IC50 > 10000.0 nM -
CHEMBL367694 IC50 > 10000.0 nM -