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Assay Detail

CHEMBL818976

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Functional
Evaluated for the inhibition of tubulin polymerization without pre-incubation
6
Total Activities
6
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. 139. Synthesis and biological evaluation of thiocolchicine analogs 5,6-dihydro-6(S)-(acyloxy)- and 5,6-dihydro-6(S)-[(aroyloxy)methyl]-1,2,3-trimethoxy-9-(methylthio)-8H- cyclohepta[a]naphthalen-8-ones as novel cytotoxic and antimitotic agents.
Sun L, McPhail AT, Hamel E, Lin CM, Hastie SB, Chang JJ, Lee KH.
J Med Chem (1993) 36 : 544 -551
PubMed 8496935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.43 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL153629 1 5.55
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.50
CHEMBL3085279 1 5.43
CHEMBL291198 1 5.42
CHEMBL357350 1 5.37
CHEMBL18981 THIOCOLCHICINE 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL153629 IC50 = 2800.0 nM 5.55
CHEMBL67 COMBRETASTATIN A4 IC50 = 3200.0 nM 5.50
CHEMBL3085279 IC50 = 3700.0 nM 5.43
CHEMBL291198 IC50 = 3800.0 nM 5.42
CHEMBL357350 IC50 = 4300.0 nM 5.37
CHEMBL18981 THIOCOLCHICINE IC50 = 4900.0 nM 5.31