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Assay Detail

CHEMBL867154

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Functional
Inhibition of tubulin polymerization
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tubulin (CHEMBL2095182)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and activity in tumor cell lines.
Ouyang X, Piatnitski EL, Pattaropong V, Chen X, He HY, Kiselyov AS, Velankar A, Kawakami J, Labelle M, Smith L, Lohman J, Lee SP, Malikzay A, Fleming J, Gerlak J, Wang Y, Rosler RL, Zhou K, Mitelman S, Camara M, Surguladze D, Doody JF, Tuma MC.
Bioorg Med Chem Lett (2006) 16 : 1191 -1196
PubMed 16377187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.55 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203642 1 6.30
CHEMBL203755 1 6.16
CHEMBL203062 1 6.16
CHEMBL204710 1 6.00
CHEMBL203974 1 5.92
CHEMBL204241 1 5.85
CHEMBL383751 1 5.82
CHEMBL381405 1 5.80
CHEMBL381122 1 5.77
CHEMBL383065 1 5.77
CHEMBL205124 1 5.75
CHEMBL205166 1 5.72
CHEMBL379249 1 5.70
CHEMBL204180 1 5.70
CHEMBL205122 1 5.70
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.68
CHEMBL203868 1 5.66
CHEMBL381961 1 5.66
CHEMBL204093 1 5.62
CHEMBL381963 1 5.47
CHEMBL203704 1 5.42
CHEMBL381049 1 5.36
CHEMBL382558 1 5.31
CHEMBL204811 1 5.30
CHEMBL382359 1 5.06
CHEMBL382358 1 5.02
CHEMBL382619 1 4.88
CHEMBL426842 1 4.81
CHEMBL383230 1 4.74
CHEMBL204754 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203642 IC50 = 500.0 nM 6.30
CHEMBL203755 IC50 = 700.0 nM 6.16
CHEMBL203062 IC50 = 700.0 nM 6.16
CHEMBL204710 IC50 = 1000.0 nM 6.00
CHEMBL203974 IC50 = 1200.0 nM 5.92
CHEMBL204241 IC50 = 1400.0 nM 5.85
CHEMBL383751 IC50 = 1500.0 nM 5.82
CHEMBL381405 IC50 = 1600.0 nM 5.80
CHEMBL381122 IC50 = 1700.0 nM 5.77
CHEMBL383065 IC50 = 1700.0 nM 5.77
CHEMBL205124 IC50 = 1800.0 nM 5.75
CHEMBL205166 IC50 = 1900.0 nM 5.72
CHEMBL379249 IC50 = 2000.0 nM 5.70
CHEMBL204180 IC50 = 2000.0 nM 5.70
CHEMBL205122 IC50 = 2000.0 nM 5.70
CHEMBL67 COMBRETASTATIN A4 IC50 = 2100.0 nM 5.68
CHEMBL203868 IC50 = 2200.0 nM 5.66
CHEMBL381961 IC50 = 2200.0 nM 5.66
CHEMBL204093 IC50 = 2400.0 nM 5.62
CHEMBL381963 IC50 = 3400.0 nM 5.47
CHEMBL203704 IC50 = 3800.0 nM 5.42
CHEMBL381049 IC50 = 4400.0 nM 5.36
CHEMBL382558 IC50 = 4900.0 nM 5.31
CHEMBL204811 IC50 = 5000.0 nM 5.30
CHEMBL382359 IC50 = 8800.0 nM 5.06
CHEMBL382358 IC50 = 9600.0 nM 5.02
CHEMBL382619 IC50 = 13300.0 nM 4.88
CHEMBL426842 IC50 = 15500.0 nM 4.81
CHEMBL383230 IC50 = 18100.0 nM 4.74
CHEMBL204754 IC50 = 29900.0 nM 4.52
CHEMBL204853 IC50 > 30000.0 nM -
CHEMBL381330 IC50 > 30000.0 nM -
CHEMBL428647 PACLITAXEL IC50 - -
CHEMBL203159 IC50 > 30000.0 nM -
CHEMBL204972 IC50 > 30000.0 nM -
CHEMBL382867 IC50 > 30000.0 nM -
CHEMBL204233 IC50 > 30000.0 nM -
CHEMBL383032 IC50 > 30000.0 nM -