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Assay Detail

CHEMBL818977

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

Functional
Inhibition of polymerization of purified bovine tubulin
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Expert

Target

Tubulin (CHEMBL2111464)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.
Wang Z, Yang D, Mohanakrishnan AK, Fanwick PE, Nampoothiri P, Hamel E, Cushman M.
J Med Chem (2000) 43 : 2419 -2429
PubMed 10882369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.17 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627442 1 6.18
CHEMBL78894 1 6.07
CHEMBL78844 1 6.01
CHEMBL299613 2-METHOXYESTRADIOL 2.0 1 5.85
CHEMBL1627880 1 5.52
CHEMBL310910 1 5.26
CHEMBL310453 1 5.16
CHEMBL311173 1 5.09
CHEMBL302676 1 4.52
CHEMBL82187 1 4.24
CHEMBL78389 1 4.10
CHEMBL81116 1 4.00
CHEMBL432546 1 -
CHEMBL310615 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627442 IC50 = 660.0 nM 6.18
CHEMBL78894 IC50 = 850.0 nM 6.07
CHEMBL78844 IC50 = 970.0 nM 6.01
CHEMBL299613 2-METHOXYESTRADIOL IC50 = 1400.0 nM 5.85
CHEMBL1627880 IC50 = 3000.0 nM 5.52
CHEMBL310910 IC50 = 5500.0 nM 5.26
CHEMBL310453 IC50 = 6900.0 nM 5.16
CHEMBL311173 IC50 = 8100.0 nM 5.09
CHEMBL302676 IC50 = 30000.0 nM 4.52
CHEMBL82187 IC50 = 57000.0 nM 4.24
CHEMBL78389 IC50 = 80000.0 nM 4.10
CHEMBL81116 IC50 = 99000.0 nM 4.00
CHEMBL432546 IC50 = 130000.0 nM -
CHEMBL310615 IC50 > 400000.0 nM -