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Assay Detail

CHEMBL4140789

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

Binding
Inhibition of tubulin polymerization (unknown origin) preincubated for 10 mins followed by GTP addition measured after 20 mins by Coomassie blue staining based SDS-PAGE analysis
22
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Intermediate

Target

Tubulin (CHEMBL2095182)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics.
Briguglio I, Laurini E, Pirisi MA, Piras S, Corona P, Fermeglia M, Pricl S, Carta A.
Eur J Med Chem (2017) 141 : 460 -472
PubMed 29055869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.61 6.82
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376464 1 6.82
CHEMBL61 PODOFILOX 4.0 1 6.58
CHEMBL9514 NOCODAZOLE 2.0 1 6.09
CHEMBL107 COLCHICINE 4.0 1 5.88
CHEMBL4174684 2 4.76
CHEMBL4163335 1 4.62
CHEMBL4174066 1 4.54
CHEMBL4171238 1 -
CHEMBL4159962 1 -
CHEMBL4167882 1 -
CHEMBL4175091 1 -
CHEMBL4162707 1 -
CHEMBL4170633 1 -
CHEMBL4159334 1 -
CHEMBL4167247 1 -
CHEMBL4169577 1 -
CHEMBL4177429 1 -
CHEMBL4166148 1 -
CHEMBL4161042 1 -
CHEMBL4171645 1 -
CHEMBL4164453 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376464 IC50 = 150.0 nM 6.82
CHEMBL61 PODOFILOX IC50 = 260.0 nM 6.58
CHEMBL9514 NOCODAZOLE IC50 = 810.0 nM 6.09
CHEMBL107 COLCHICINE IC50 = 1320.0 nM 5.88
CHEMBL4174684 IC50 = 17200.0 nM 4.76
CHEMBL4163335 IC50 = 23900.0 nM 4.62
CHEMBL4174066 IC50 = 29100.0 nM 4.54
CHEMBL4175091 IC50 > 30000.0 nM -
CHEMBL4164453 IC50 > 30000.0 nM -
CHEMBL4171645 IC50 > 30000.0 nM -
CHEMBL4161042 IC50 > 30000.0 nM -
CHEMBL4166148 IC50 > 30000.0 nM -
CHEMBL4177429 IC50 > 30000.0 nM -
CHEMBL4167882 IC50 > 30000.0 nM -
CHEMBL4167247 IC50 > 30000.0 nM -
CHEMBL4159334 IC50 > 30000.0 nM -
CHEMBL4170633 IC50 > 30000.0 nM -
CHEMBL4162707 IC50 > 30000.0 nM -
CHEMBL4159962 IC50 > 30000.0 nM -
CHEMBL4171238 IC50 > 30000.0 nM -
CHEMBL4174684 Inhibition - % -
CHEMBL4169577 IC50 > 30000.0 nM -