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Assay Detail

CHEMBL815033

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

Functional
Inhibition of tubulin polymerization with preincubation for 15 minutes at 37 degree Centigrade prior to addition of the GTP required for polymerization
17
Total Activities
17
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 17 5.46 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18981 THIOCOLCHICINE 1 5.68
CHEMBL153629 1 5.62
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.54
CHEMBL291198 1 5.52
CHEMBL346889 1 5.47
CHEMBL150672 1 5.47
CHEMBL3085279 1 5.44
CHEMBL357350 1 5.43
CHEMBL107 COLCHICINE 4.0 1 5.38
CHEMBL153743 1 5.35
CHEMBL153593 1 5.18
CHEMBL149532 1 -
CHEMBL52536 1 -
CHEMBL51766 1 -
CHEMBL150611 1 -
CHEMBL431151 1 -
CHEMBL346395 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18981 THIOCOLCHICINE IC50 = 2100.0 nM 5.68
CHEMBL153629 IC50 = 2400.0 nM 5.62
CHEMBL67 COMBRETASTATIN A4 IC50 = 2900.0 nM 5.54
CHEMBL291198 IC50 = 3000.0 nM 5.52
CHEMBL346889 IC50 = 3400.0 nM 5.47
CHEMBL150672 IC50 = 3400.0 nM 5.47
CHEMBL3085279 IC50 = 3600.0 nM 5.44
CHEMBL357350 IC50 = 3700.0 nM 5.43
CHEMBL107 COLCHICINE IC50 = 4200.0 nM 5.38
CHEMBL153743 IC50 = 4500.0 nM 5.35
CHEMBL153593 IC50 = 6600.0 nM 5.18
CHEMBL149532 IC50 > 40000.0 nM -
CHEMBL52536 IC50 > 40000.0 nM -
CHEMBL51766 IC50 > 40000.0 nM -
CHEMBL150611 IC50 > 40000.0 nM -
CHEMBL431151 IC50 > 40000.0 nM -
CHEMBL346395 IC50 > 40000.0 nM -