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Assay Detail

CHEMBL921472

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

Binding
Inhibition of rat brain tubulin polymerization
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tubulysin analogs incorporating desmethyl and dimethyl tubuphenylalanine derivatives.
Balasubramanian R, Raghavan B, Steele JC, Sackett DL, Fecik RA.
Bioorg Med Chem Lett (2008) 18 : 2996 -2999
PubMed 18411048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.97 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182319 TALTOBULIN 2.0 1 9.15
CHEMBL554150 1 6.22
CHEMBL256922 TUBULYSIN-A 1 6.12
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.96
CHEMBL536094 1 5.82
CHEMBL536768 1 5.64
CHEMBL536093 1 5.57
CHEMBL535866 1 5.36
CHEMBL535642 1 4.96
CHEMBL536315 1 4.89
CHEMBL541395 1 -
CHEMBL558772 1 -
CHEMBL541650 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182319 TALTOBULIN IC50 = 0.7 nM 9.15
CHEMBL554150 IC50 = 600.0 nM 6.22
CHEMBL256922 TUBULYSIN-A IC50 = 750.0 nM 6.12
CHEMBL67 COMBRETASTATIN A4 IC50 = 1100.0 nM 5.96
CHEMBL536094 IC50 = 1500.0 nM 5.82
CHEMBL536768 IC50 = 2300.0 nM 5.64
CHEMBL536093 IC50 = 2700.0 nM 5.57
CHEMBL535866 IC50 = 4400.0 nM 5.36
CHEMBL535642 IC50 = 11000.0 nM 4.96
CHEMBL536315 IC50 = 13000.0 nM 4.89
CHEMBL541395 IC50 > 20000.0 nM -
CHEMBL558772 IC50 > 20000.0 nM -
CHEMBL541650 IC50 > 20000.0 nM -