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Assay Detail

CHEMBL1055772

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Binding
Inhibition of bovine brain tubulin polymerization
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
Putey A, Popowycz F, Do QT, Bernard P, Talapatra SK, Kozielski F, Galmarini CM, Joseph B.
J Med Chem (2009) 52 : 5916 -5925
PubMed 19743863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.30 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140220 1 6.28
CHEMBL49642 INDIBULIN 2.0 1 6.00
CHEMBL558718 1 5.43
CHEMBL559349 1 5.36
CHEMBL525978 1 5.28
CHEMBL538707 1 5.27
CHEMBL562730 1 5.21
CHEMBL550404 1 5.21
CHEMBL562903 1 5.11
CHEMBL550809 1 5.05
CHEMBL562645 1 5.04
CHEMBL541706 1 4.89
CHEMBL552568 1 4.83
CHEMBL550529 1 -
CHEMBL552278 1 -
CHEMBL564070 1 -
CHEMBL559747 1 -
CHEMBL562972 1 -
CHEMBL559119 1 -
CHEMBL557827 1 -
CHEMBL559202 1 -
CHEMBL563170 1 -
CHEMBL556208 1 -
CHEMBL559028 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140220 IC50 = 530.0 nM 6.28
CHEMBL49642 INDIBULIN IC50 = 1000.0 nM 6.00
CHEMBL558718 IC50 = 3700.0 nM 5.43
CHEMBL559349 IC50 = 4400.0 nM 5.36
CHEMBL525978 IC50 = 5300.0 nM 5.28
CHEMBL538707 IC50 = 5400.0 nM 5.27
CHEMBL562730 IC50 = 6100.0 nM 5.21
CHEMBL550404 IC50 = 6200.0 nM 5.21
CHEMBL562903 IC50 = 7700.0 nM 5.11
CHEMBL550809 IC50 = 9000.0 nM 5.05
CHEMBL562645 IC50 = 9100.0 nM 5.04
CHEMBL541706 IC50 = 13000.0 nM 4.89
CHEMBL552568 IC50 = 14900.0 nM 4.83
CHEMBL550529 IC50 - -
CHEMBL552278 IC50 - -
CHEMBL564070 IC50 - -
CHEMBL559747 IC50 - -
CHEMBL562972 IC50 - -
CHEMBL559119 IC50 - -
CHEMBL557827 IC50 - -
CHEMBL559202 IC50 - -
CHEMBL563170 IC50 - -
CHEMBL556208 IC50 - -
CHEMBL559028 IC50 - -