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Assay Detail

CHEMBL3372544

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

Binding
Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry
40
Total Activities
40
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

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 40 5.65 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318106 1 6.07
CHEMBL3318112 1 6.05
CHEMBL3318111 1 6.02
CHEMBL3318091 1 6.00
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.00
CHEMBL3318102 1 6.00
CHEMBL3318115 1 5.92
CHEMBL3318119 1 5.92
CHEMBL3318105 1 5.92
CHEMBL3318123 1 5.89
CHEMBL3318122 1 5.89
CHEMBL3318101 1 5.89
CHEMBL3318095 1 5.85
CHEMBL3318100 1 5.85
CHEMBL3318104 1 5.82
CHEMBL3318085 1 5.82
CHEMBL3318125 1 5.77
CHEMBL3318118 1 5.77
CHEMBL3318114 1 5.75
CHEMBL3318094 1 5.68
CHEMBL3318124 1 5.68
CHEMBL3318089 1 5.66
CHEMBL3318090 1 5.64
CHEMBL3318108 1 5.60
CHEMBL3318092 1 5.60
CHEMBL3318107 1 5.60
CHEMBL3318103 1 5.60
CHEMBL3318113 1 5.57
CHEMBL107 COLCHICINE 4.0 1 5.50
CHEMBL3318116 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318106 IC50 = 860.0 nM 6.07
CHEMBL3318112 IC50 = 900.0 nM 6.05
CHEMBL3318111 IC50 = 950.0 nM 6.02
CHEMBL3318091 IC50 = 1000.0 nM 6.00
CHEMBL67 COMBRETASTATIN A4 IC50 = 1000.0 nM 6.00
CHEMBL3318102 IC50 = 1000.0 nM 6.00
CHEMBL3318115 IC50 = 1200.0 nM 5.92
CHEMBL3318119 IC50 = 1200.0 nM 5.92
CHEMBL3318105 IC50 = 1200.0 nM 5.92
CHEMBL3318101 IC50 = 1300.0 nM 5.89
CHEMBL3318122 IC50 = 1300.0 nM 5.89
CHEMBL3318123 IC50 = 1300.0 nM 5.89
CHEMBL3318095 IC50 = 1400.0 nM 5.85
CHEMBL3318100 IC50 = 1400.0 nM 5.85
CHEMBL3318085 IC50 = 1500.0 nM 5.82
CHEMBL3318104 IC50 = 1500.0 nM 5.82
CHEMBL3318125 IC50 = 1700.0 nM 5.77
CHEMBL3318118 IC50 = 1700.0 nM 5.77
CHEMBL3318114 IC50 = 1800.0 nM 5.75
CHEMBL3318124 IC50 = 2100.0 nM 5.68
CHEMBL3318094 IC50 = 2100.0 nM 5.68
CHEMBL3318089 IC50 = 2200.0 nM 5.66
CHEMBL3318090 IC50 = 2300.0 nM 5.64
CHEMBL3318108 IC50 = 2500.0 nM 5.60
CHEMBL3318092 IC50 = 2500.0 nM 5.60
CHEMBL3318107 IC50 = 2500.0 nM 5.60
CHEMBL3318103 IC50 = 2500.0 nM 5.60
CHEMBL3318113 IC50 = 2700.0 nM 5.57
CHEMBL107 COLCHICINE IC50 = 3200.0 nM 5.50
CHEMBL3318116 IC50 = 6100.0 nM 5.21
CHEMBL3318099 IC50 = 6800.0 nM 5.17
CHEMBL3318088 IC50 = 8800.0 nM 5.06
CHEMBL3318097 IC50 = 8900.0 nM 5.05
CHEMBL3318110 IC50 = 13000.0 nM 4.89
CHEMBL3318120 IC50 = 15000.0 nM 4.82
CHEMBL3318131 IC50 = 16000.0 nM 4.80
CHEMBL3318127 IC50 > 40000.0 nM -
CHEMBL3318130 IC50 > 40000.0 nM -
CHEMBL3318087 IC50 > 40000.0 nM -
CHEMBL3318086 IC50 > 40000.0 nM -