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Assay Detail

CHEMBL815870

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Functional
Evaluated for inhibition of tubulin polymerization.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Tubulin (CHEMBL2094134)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Synthesis of analogs of 2-methoxyestradiol with enhanced inhibitory effects on tubulin polymerization and cancer cell growth.
Cushman M, He HM, Katzenellenbogen JA, Varma RK, Hamel E, Lin CM, Ram S, Sachdeva YP.
J Med Chem (1997) 40 : 2323 -2334
PubMed 9240348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.45 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627442 1 5.89
CHEMBL1627875 1 5.82
CHEMBL1627475 1 5.54
CHEMBL299613 2-METHOXYESTRADIOL 2.0 1 5.51
CHEMBL1627880 1 5.39
CHEMBL1627463 1 5.37
CHEMBL77320 1 5.36
CHEMBL1627461 1 5.32
CHEMBL1627882 1 5.23
CHEMBL1627888 1 5.06
CHEMBL1627467 1 -
CHEMBL1627462 1 -
CHEMBL1627891 1 -
CHEMBL1627468 1 -
CHEMBL1627466 1 -
CHEMBL1627472 1 -
CHEMBL1627474 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627442 IC50 = 1300.0 nM 5.89
CHEMBL1627875 IC50 = 1500.0 nM 5.82
CHEMBL1627475 IC50 = 2900.0 nM 5.54
CHEMBL299613 2-METHOXYESTRADIOL IC50 = 3100.0 nM 5.51
CHEMBL1627880 IC50 = 4100.0 nM 5.39
CHEMBL1627463 IC50 = 4300.0 nM 5.37
CHEMBL77320 IC50 = 4400.0 nM 5.36
CHEMBL1627461 IC50 = 4800.0 nM 5.32
CHEMBL1627882 IC50 = 5900.0 nM 5.23
CHEMBL1627888 IC50 = 8800.0 nM 5.06
CHEMBL1627467 IC50 > 40000.0 nM -
CHEMBL1627462 IC50 > 40000.0 nM -
CHEMBL1627891 IC50 > 40000.0 nM -
CHEMBL1627468 IC50 > 40000.0 nM -
CHEMBL1627466 IC50 > 40000.0 nM -
CHEMBL1627472 IC50 > 40000.0 nM -
CHEMBL1627474 IC50 > 40000.0 nM -