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Assay Detail

CHEMBL4028773

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

Functional
Cytotoxicity against human DU145-TxR cells after 72 hrs by MTS assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type DU145-TxR
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Heterocyclic-Fused Pyrimidines as Novel Tubulin Polymerization Inhibitors Targeting the Colchicine Binding Site: Structural Basis and Antitumor Efficacy.
Banerjee S, Arnst KE, Wang Y, Kumar G, Deng S, Yang L, Li GB, Yang J, White SW, Li W, Miller DD.
J Med Chem (2018) 61 : 1704 -1718
PubMed 29406710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.08 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102788 1 7.70
CHEMBL92 DOCETAXEL ANHYDROUS 4.0 1 6.45
CHEMBL107 COLCHICINE 4.0 1 -
CHEMBL428647 PACLITAXEL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102788 IC50 = 19.9 nM 7.70
CHEMBL92 DOCETAXEL ANHYDROUS IC50 = 352.3 nM 6.45
CHEMBL107 COLCHICINE IC50 > 1000.0 nM -
CHEMBL428647 PACLITAXEL IC50 > 1000.0 nM -