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Assay Detail

CHEMBL832453

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Binding
Concentration required for 50% inhibition of tubulin polymerization
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Tubulin beta-1 chain (CHEMBL1915) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quantitative structure-activity relationship (5D-QSAR) study of combretastatin-like analogues as inhibitors of tubulin assembly.
Ducki S, Mackenzie G, Lawrence NJ, Snyder JP.
J Med Chem (2005) 48 : 457 -465
PubMed 15658859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 5.73 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370250 — — 1 6.92
CHEMBL195572 — — 1 6.89
CHEMBL193716 — — 1 6.89
CHEMBL67 COMBRETASTATIN A4 -1.0 1 6.75
CHEMBL47426 — — 1 6.70
CHEMBL195840 — — 1 6.35
CHEMBL9859 — — 1 6.34
CHEMBL371839 — — 1 6.33
CHEMBL192739 — — 1 6.30
CHEMBL364034 — — 1 6.29
CHEMBL150582 — — 1 6.25
CHEMBL9941 — — 1 6.21
CHEMBL426644 — — 1 6.19
CHEMBL192540 — — 1 6.19
CHEMBL192056 — — 1 6.16
CHEMBL193038 — — 1 5.92
CHEMBL192357 — — 1 5.92
CHEMBL195158 — — 1 5.90
CHEMBL191747 — — 1 5.89
CHEMBL194925 — — 1 5.77
CHEMBL427543 — — 1 5.70
CHEMBL364234 — — 1 5.70
CHEMBL195819 — — 1 5.62
CHEMBL364969 — — 1 5.60
CHEMBL191349 — — 1 5.51
CHEMBL75284 — — 1 5.47
CHEMBL193257 — — 1 5.40
CHEMBL191350 — — 1 5.35
CHEMBL195605 — — 1 5.26
CHEMBL195538 — — 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370250 — IC50 = 120.0 nM 6.92
CHEMBL195572 — IC50 = 130.0 nM 6.89
CHEMBL193716 — IC50 = 130.0 nM 6.89
CHEMBL67 COMBRETASTATIN A4 IC50 = 180.0 nM 6.75
CHEMBL47426 — IC50 = 200.0 nM 6.70
CHEMBL195840 — IC50 = 450.0 nM 6.35
CHEMBL9859 — IC50 = 460.0 nM 6.34
CHEMBL371839 — IC50 = 470.0 nM 6.33
CHEMBL192739 — IC50 = 500.0 nM 6.30
CHEMBL364034 — IC50 = 510.0 nM 6.29
CHEMBL150582 — IC50 = 560.0 nM 6.25
CHEMBL9941 — IC50 = 620.0 nM 6.21
CHEMBL192540 — IC50 = 650.0 nM 6.19
CHEMBL426644 — IC50 = 650.0 nM 6.19
CHEMBL192056 — IC50 = 700.0 nM 6.16
CHEMBL193038 — IC50 = 1200.0 nM 5.92
CHEMBL192357 — IC50 = 1200.0 nM 5.92
CHEMBL195158 — IC50 = 1250.0 nM 5.90
CHEMBL191747 — IC50 = 1300.0 nM 5.89
CHEMBL194925 — IC50 = 1700.0 nM 5.77
CHEMBL427543 — IC50 = 2000.0 nM 5.70
CHEMBL364234 — IC50 = 2000.0 nM 5.70
CHEMBL195819 — IC50 = 2400.0 nM 5.62
CHEMBL364969 — IC50 = 2500.0 nM 5.60
CHEMBL191349 — IC50 = 3100.0 nM 5.51
CHEMBL75284 — IC50 = 3400.0 nM 5.47
CHEMBL193257 — IC50 = 4000.0 nM 5.40
CHEMBL191350 — IC50 = 4500.0 nM 5.35
CHEMBL195605 — IC50 = 5500.0 nM 5.26
CHEMBL195538 — IC50 = 6600.0 nM 5.18
CHEMBL345556 — IC50 = 7200.0 nM 5.14
CHEMBL195899 — IC50 = 7900.0 nM 5.10
CHEMBL194709 — IC50 = 9000.0 nM 5.05
CHEMBL9652 — IC50 = 10000.0 nM 5.00
CHEMBL356370 — IC50 = 11000.0 nM 4.96
CHEMBL191407 — IC50 = 12000.0 nM 4.92
CHEMBL150438 — IC50 = 21000.0 nM 4.68
CHEMBL192221 — IC50 = 31000.0 nM 4.51
CHEMBL150590 — IC50 = 41000.0 nM 4.39
CHEMBL36455 E-COMBRETASTATIN A-4 IC50 = 50000.0 nM 4.30
CHEMBL192276 — IC50 > 100000.0 nM -
CHEMBL150463 — IC50 > 100000.0 nM -
CHEMBL358037 — IC50 > 100000.0 nM -
CHEMBL153243 — IC50 > 100000.0 nM -
CHEMBL126617 — IC50 > 100000.0 nM -
CHEMBL364517 — IC50 > 10000.0 nM -
CHEMBL191957 — IC50 > 10000.0 nM -