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Assay Detail

CHEMBL3376852

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

Functional
Cytotoxicity against human MESSA/DX5 cells assessed as growth inhibition after 72 hrs by CellTitre-Glo assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MES-SA/Dx5
Confidence 1 — Organism
Curated By Autocuration

Publication

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.
La Regina G, Bai R, Coluccia A, Famiglini V, Pelliccia S, Passacantilli S, Mazzoccoli C, Ruggieri V, Sisinni L, Bolognesi A, Rensen WM, Miele A, Nalli M, Alfonsi R, Di Marcotullio L, Gulino A, Brancale A, Novellino E, Dondio G, Vultaggio S, Varasi M, Mercurio C, Hamel E, Lavia P, Silvestri R.
J Med Chem (2014) 57 : 6531 -6552
PubMed 25025991 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.05 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 8.59
CHEMBL3318100 1 8.34
CHEMBL3318105 1 7.80
CHEMBL3318085 1 7.12
CHEMBL3318115 1 7.06
CHEMBL159 VINBLASTINE 4.0 1 6.84
CHEMBL107 COLCHICINE 4.0 1 6.48
CHEMBL3318114 1 6.33
CHEMBL3318113 1 6.18
CHEMBL428647 PACLITAXEL 4.0 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 2.6 nM 8.59
CHEMBL3318100 IC50 = 4.6 nM 8.34
CHEMBL3318105 IC50 = 16.0 nM 7.80
CHEMBL3318085 IC50 = 76.0 nM 7.12
CHEMBL3318115 IC50 = 87.0 nM 7.06
CHEMBL159 VINBLASTINE IC50 = 144.0 nM 6.84
CHEMBL107 COLCHICINE IC50 = 329.0 nM 6.48
CHEMBL3318114 IC50 = 471.0 nM 6.33
CHEMBL3318113 IC50 = 653.0 nM 6.18
CHEMBL428647 PACLITAXEL IC50 = 1764.0 nM 5.75