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Assay Detail

CHEMBL2321170

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

Binding
Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry
ChEMBL ↗
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tubulin (CHEMBL2095182) ↗
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.
La Regina G, Bai R, Rensen WM, Di Cesare E, Coluccia A, Piscitelli F, Famiglini V, Reggio A, Nalli M, Pelliccia S, Da Pozzo E, Costa B, Granata I, Porta A, Maresca B, Soriani A, Iannitto ML, Santoni A, Li J, Miranda Cona M, Chen F, Ni Y, Brancale A, Dondio G, Vultaggio S, Varasi M, Mercurio C, Martini C, Hamel E, Lavia P, Novellino E, Silvestri R.
J Med Chem (2013) 56 : 123 -149
PubMed 23214452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 5.58 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2313489 — — 1 6.04
CHEMBL2313462 — — 1 6.03
CHEMBL2313809 — — 1 6.03
CHEMBL2313799 — — 1 6.02
CHEMBL2313472 — — 1 6.02
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.00
CHEMBL2313477 — — 1 6.00
CHEMBL2313464 — — 1 5.96
CHEMBL2313795 — — 1 5.96
CHEMBL2313792 — — 1 5.92
CHEMBL2313788 — — 1 5.92
CHEMBL2313790 — — 1 5.89
CHEMBL2313470 — — 1 5.89
CHEMBL2313819 — — 1 5.85
CHEMBL2313468 — — 1 5.82
CHEMBL2313452 — — 1 5.82
CHEMBL2313787 — — 1 5.77
CHEMBL2313813 — — 1 5.77
CHEMBL2313811 — — 1 5.77
CHEMBL2313453 — — 1 5.77
CHEMBL2313815 — — 1 5.75
CHEMBL2313810 — — 1 5.75
CHEMBL2313820 — — 1 5.75
CHEMBL2313485 — — 1 5.75
CHEMBL2313483 — — 1 5.75
CHEMBL2313793 — — 1 5.72
CHEMBL2313456 — — 1 5.70
CHEMBL2313797 — — 1 5.68
CHEMBL2313812 — — 1 5.68
CHEMBL2313458 — — 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2313489 — IC50 = 920.0 nM 6.04
CHEMBL2313462 — IC50 = 940.0 nM 6.03
CHEMBL2313809 — IC50 = 940.0 nM 6.03
CHEMBL2313799 — IC50 = 960.0 nM 6.02
CHEMBL2313472 — IC50 = 950.0 nM 6.02
CHEMBL67 COMBRETASTATIN A4 IC50 = 1000.0 nM 6.00
CHEMBL2313477 — IC50 = 1000.0 nM 6.00
CHEMBL2313464 — IC50 = 1100.0 nM 5.96
CHEMBL2313795 — IC50 = 1100.0 nM 5.96
CHEMBL2313792 — IC50 = 1200.0 nM 5.92
CHEMBL2313788 — IC50 = 1200.0 nM 5.92
CHEMBL2313790 — IC50 = 1300.0 nM 5.89
CHEMBL2313470 — IC50 = 1300.0 nM 5.89
CHEMBL2313819 — IC50 = 1400.0 nM 5.85
CHEMBL2313452 — IC50 = 1500.0 nM 5.82
CHEMBL2313468 — IC50 = 1500.0 nM 5.82
CHEMBL2313787 — IC50 = 1700.0 nM 5.77
CHEMBL2313813 — IC50 = 1700.0 nM 5.77
CHEMBL2313811 — IC50 = 1700.0 nM 5.77
CHEMBL2313453 — IC50 = 1700.0 nM 5.77
CHEMBL2313815 — IC50 = 1800.0 nM 5.75
CHEMBL2313810 — IC50 = 1800.0 nM 5.75
CHEMBL2313820 — IC50 = 1800.0 nM 5.75
CHEMBL2313485 — IC50 = 1800.0 nM 5.75
CHEMBL2313483 — IC50 = 1800.0 nM 5.75
CHEMBL2313793 — IC50 = 1900.0 nM 5.72
CHEMBL2313456 — IC50 = 2000.0 nM 5.70
CHEMBL2313797 — IC50 = 2100.0 nM 5.68
CHEMBL2313812 — IC50 = 2100.0 nM 5.68
CHEMBL2313458 — IC50 = 2600.0 nM 5.58
CHEMBL2313798 — IC50 = 2700.0 nM 5.57
CHEMBL2313457 — IC50 = 2800.0 nM 5.55
CHEMBL2313488 — IC50 = 3000.0 nM 5.52
CHEMBL2313482 — IC50 = 3100.0 nM 5.51
CHEMBL107 COLCHICINE IC50 = 3200.0 nM 5.50
CHEMBL2313800 — IC50 = 3300.0 nM 5.48
CHEMBL2313817 — IC50 = 3300.0 nM 5.48
CHEMBL2313806 — IC50 = 3300.0 nM 5.48
CHEMBL2313804 — IC50 = 3400.0 nM 5.47
CHEMBL2313791 — IC50 = 3500.0 nM 5.46
CHEMBL2313818 — IC50 = 3600.0 nM 5.44
CHEMBL2313808 — IC50 = 3700.0 nM 5.43
CHEMBL2313459 — IC50 = 4000.0 nM 5.40
CHEMBL2313481 — IC50 = 4000.0 nM 5.40
CHEMBL2313466 — IC50 = 4100.0 nM 5.39
CHEMBL2313803 — IC50 = 4500.0 nM 5.35
CHEMBL2313789 — IC50 = 4600.0 nM 5.34
CHEMBL2313807 — IC50 = 5700.0 nM 5.24
CHEMBL2313473 — IC50 = 6000.0 nM 5.22
CHEMBL2313471 — IC50 = 6300.0 nM 5.20