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Assay Detail

CHEMBL845250

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

Functional
Concentration needed to inhibit tubulin polymerization by 50%
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tubulin beta chain (CHEMBL3394)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
Wang L, Woods KW, Li Q, Barr KJ, McCroskey RW, Hannick SM, Gherke L, Credo RB, Hui YH, Marsh K, Warner R, Lee JY, Zielinski-Mozng N, Frost D, Rosenberg SH, Sham HL.
J Med Chem (2002) 45 : 1697 -1711
PubMed 11931625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.43 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45512 1 6.17
CHEMBL297848 1 6.14
CHEMBL297677 1 6.10
CHEMBL296066 1 6.06
CHEMBL46052 1 6.04
CHEMBL45473 1 6.01
CHEMBL295738 1 5.96
CHEMBL67 COMBRETASTATIN A4 -1.0 1 5.92
CHEMBL47306 1 5.75
CHEMBL295644 1 5.70
CHEMBL296914 1 5.55
CHEMBL296406 1 5.43
CHEMBL46072 1 5.12
CHEMBL45481 1 5.11
CHEMBL297236 1 4.64
CHEMBL46215 1 4.51
CHEMBL47112 1 4.46
CHEMBL45469 1 4.32
CHEMBL48004 1 4.15
CHEMBL297018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45512 IC50 = 680.0 nM 6.17
CHEMBL297848 IC50 = 730.0 nM 6.14
CHEMBL297677 IC50 = 790.0 nM 6.10
CHEMBL296066 IC50 = 870.0 nM 6.06
CHEMBL46052 IC50 = 920.0 nM 6.04
CHEMBL45473 IC50 = 980.0 nM 6.01
CHEMBL295738 IC50 = 1100.0 nM 5.96
CHEMBL67 COMBRETASTATIN A4 IC50 = 1200.0 nM 5.92
CHEMBL47306 IC50 = 1800.0 nM 5.75
CHEMBL295644 IC50 = 2000.0 nM 5.70
CHEMBL296914 IC50 = 2800.0 nM 5.55
CHEMBL296406 IC50 = 3700.0 nM 5.43
CHEMBL46072 IC50 = 7600.0 nM 5.12
CHEMBL45481 IC50 = 7700.0 nM 5.11
CHEMBL297236 IC50 = 23000.0 nM 4.64
CHEMBL46215 IC50 = 31000.0 nM 4.51
CHEMBL47112 IC50 = 35000.0 nM 4.46
CHEMBL45469 IC50 = 48000.0 nM 4.32
CHEMBL48004 IC50 = 71000.0 nM 4.15
CHEMBL297018 IC50 = 130000.0 nM -