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Assay Detail

CHEMBL820777

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Functional
Inhibition of tubulin polymerization
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2094134)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Antitumor agents. 178. Synthesis and biological evaluation of substituted 2-aryl-1,8-naphthyridin-4(1H)-ones as antitumor agents that inhibit tubulin polymerization.
Chen K, Kuo SC, Hsieh MC, Mauger A, Lin CM, Hamel E, Lee KH.
J Med Chem (1997) 40 : 3049 -3056
PubMed 9301667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.91 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61 PODOFILOX 4.0 1 6.34
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.28
CHEMBL51928 1 6.28
CHEMBL50666 1 6.26
CHEMBL48300 1 6.20
CHEMBL52342 1 6.18
CHEMBL49827 1 6.14
CHEMBL295291 1 6.13
CHEMBL51408 1 6.11
CHEMBL49835 1 6.11
CHEMBL107 COLCHICINE 4.0 1 6.10
CHEMBL51139 1 6.05
CHEMBL51998 1 6.03
CHEMBL105469 1 6.00
CHEMBL423845 1 5.96
CHEMBL45677 1 5.82
CHEMBL49016 1 5.82
CHEMBL48330 1 5.75
CHEMBL317272 1 5.75
CHEMBL45620 1 5.72
CHEMBL50866 1 5.68
CHEMBL102019 1 5.64
CHEMBL48541 1 5.60
CHEMBL299979 1 5.48
CHEMBL48779 1 5.29
CHEMBL298328 1 4.85
CHEMBL440887 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61 PODOFILOX IC50 = 460.0 nM 6.34
CHEMBL67 COMBRETASTATIN A4 IC50 = 530.0 nM 6.28
CHEMBL51928 IC50 = 530.0 nM 6.28
CHEMBL50666 IC50 = 550.0 nM 6.26
CHEMBL48300 IC50 = 630.0 nM 6.20
CHEMBL52342 IC50 = 660.0 nM 6.18
CHEMBL49827 IC50 = 720.0 nM 6.14
CHEMBL295291 IC50 = 740.0 nM 6.13
CHEMBL51408 IC50 = 770.0 nM 6.11
CHEMBL49835 IC50 = 780.0 nM 6.11
CHEMBL107 COLCHICINE IC50 = 800.0 nM 6.10
CHEMBL51139 IC50 = 890.0 nM 6.05
CHEMBL51998 IC50 = 930.0 nM 6.03
CHEMBL105469 IC50 = 1000.0 nM 6.00
CHEMBL423845 IC50 = 1100.0 nM 5.96
CHEMBL45677 IC50 = 1500.0 nM 5.82
CHEMBL49016 IC50 = 1500.0 nM 5.82
CHEMBL48330 IC50 = 1800.0 nM 5.75
CHEMBL317272 IC50 = 1800.0 nM 5.75
CHEMBL45620 IC50 = 1900.0 nM 5.72
CHEMBL50866 IC50 = 2100.0 nM 5.68
CHEMBL102019 IC50 = 2300.0 nM 5.64
CHEMBL48541 IC50 = 2500.0 nM 5.60
CHEMBL299979 IC50 = 3300.0 nM 5.48
CHEMBL48779 IC50 = 5100.0 nM 5.29
CHEMBL298328 IC50 = 14000.0 nM 4.85
CHEMBL440887 IC50 > 40000.0 nM -