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Assay Detail

CHEMBL3100255

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

Functional
Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by coulter counting analysis
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Concise synthesis and biological evaluation of 2-Aroyl-5-amino benzo[b]thiophene derivatives as a novel class of potent antimitotic agents.
Romagnoli R, Baraldi PG, Lopez-Cara C, Preti D, Aghazadeh Tabrizi M, Balzarini J, Bassetto M, Brancale A, Fu XH, Gao Y, Li J, Zhang SZ, Hamel E, Bortolozzi R, Basso G, Viola G.
J Med Chem (2013) 56 : 9296 -9309
PubMed 24164557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.86 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 8.72
CHEMBL3099862 1 8.10
CHEMBL3099860 1 7.89
CHEMBL3099864 1 7.89
CHEMBL3099863 1 7.80
CHEMBL3099865 1 7.18
CHEMBL3099850 1 7.16
CHEMBL3099861 1 7.00
CHEMBL3099853 1 7.00
CHEMBL3099855 1 6.70
CHEMBL3099854 1 6.66
CHEMBL3099849 1 6.44
CHEMBL3099856 1 6.16
CHEMBL3099857 1 6.12
CHEMBL3099852 1 5.82
CHEMBL3099851 1 5.80
CHEMBL3099858 1 5.80
CHEMBL3099859 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 1.9 nM 8.72
CHEMBL3099862 IC50 = 8.0 nM 8.10
CHEMBL3099860 IC50 = 13.0 nM 7.89
CHEMBL3099864 IC50 = 13.0 nM 7.89
CHEMBL3099863 IC50 = 16.0 nM 7.80
CHEMBL3099865 IC50 = 66.0 nM 7.18
CHEMBL3099850 IC50 = 69.0 nM 7.16
CHEMBL3099861 IC50 = 100.0 nM 7.00
CHEMBL3099853 IC50 = 100.0 nM 7.00
CHEMBL3099855 IC50 = 200.0 nM 6.70
CHEMBL3099854 IC50 = 220.0 nM 6.66
CHEMBL3099849 IC50 = 360.0 nM 6.44
CHEMBL3099856 IC50 = 700.0 nM 6.16
CHEMBL3099857 IC50 = 760.0 nM 6.12
CHEMBL3099852 IC50 = 1500.0 nM 5.82
CHEMBL3099851 IC50 = 1600.0 nM 5.80
CHEMBL3099858 IC50 = 1600.0 nM 5.80
CHEMBL3099859 IC50 = 6300.0 nM 5.20