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Assay Detail

CHEMBL1026429

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

Binding
Displacement of [3H]colchicine from tubulin by scintillation proximity assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel A-ring and B-ring modified combretastatin A-4 (CA-4) analogues endowed with interesting cytotoxic activity.
Simoni D, Romagnoli R, Baruchello R, Rondanin R, Grisolia G, Eleopra M, Rizzi M, Tolomeo M, Giannini G, Alloatti D, Castorina M, Marcellini M, Pisano C.
J Med Chem (2008) 51 : 6211 -6215
PubMed 18783207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.10 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511529 1 10.70
CHEMBL462474 1 10.70
CHEMBL502484 1 10.30
CHEMBL67 COMBRETASTATIN A4 -1.0 1 10.00
CHEMBL107 COLCHICINE 4.0 1 8.77
CHEMBL447389 1 8.42
CHEMBL462056 1 8.40
CHEMBL462055 1 8.31
CHEMBL459937 1 8.21
CHEMBL509991 1 8.21
CHEMBL518818 1 8.11
CHEMBL509714 1 -
CHEMBL512217 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511529 IC50 = 0.02 nM 10.70
CHEMBL462474 IC50 = 0.02 nM 10.70
CHEMBL502484 IC50 = 0.05 nM 10.30
CHEMBL67 COMBRETASTATIN A4 IC50 = 0.1 nM 10.00
CHEMBL107 COLCHICINE IC50 = 1.7 nM 8.77
CHEMBL447389 IC50 = 3.8 nM 8.42
CHEMBL462056 IC50 = 4.0 nM 8.40
CHEMBL462055 IC50 = 4.9 nM 8.31
CHEMBL459937 IC50 = 6.2 nM 8.21
CHEMBL509991 IC50 = 6.2 nM 8.21
CHEMBL518818 IC50 = 7.7 nM 8.11
CHEMBL509714 IC50 - -
CHEMBL512217 IC50 - -