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Assay Detail

CHEMBL4028749

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

Functional
Cytotoxicity against human RPMI7951 cells after 72 hrs by MTS assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RPMI-7951
Confidence 1 — Organism
Curated By Autocuration

Target

RPMI-7951 (CHEMBL612447)
Type CELL-LINE
Organism Homo sapiens

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 16 7.53 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067605 1 8.36
CHEMBL4095025 1 8.29
CHEMBL107 COLCHICINE 4.0 1 8.18
CHEMBL4102788 1 8.09
CHEMBL4095734 1 7.75
CHEMBL4079240 1 7.38
CHEMBL4088019 1 7.32
CHEMBL4068389 1 7.23
CHEMBL4105202 1 7.04
CHEMBL4075372 1 6.75
CHEMBL4102747 1 6.39
CHEMBL4087344 1 -
CHEMBL4103488 1 -
CHEMBL4079230 1 -
CHEMBL4059730 1 -
CHEMBL4094045 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067605 IC50 = 4.4 nM 8.36
CHEMBL4095025 IC50 = 5.1 nM 8.29
CHEMBL107 COLCHICINE IC50 = 6.6 nM 8.18
CHEMBL4102788 IC50 = 8.2 nM 8.09
CHEMBL4095734 IC50 = 17.6 nM 7.75
CHEMBL4079240 IC50 = 41.9 nM 7.38
CHEMBL4088019 IC50 = 47.5 nM 7.32
CHEMBL4068389 IC50 = 58.9 nM 7.23
CHEMBL4105202 IC50 = 91.3 nM 7.04
CHEMBL4075372 IC50 = 178.9 nM 6.75
CHEMBL4102747 IC50 = 404.5 nM 6.39
CHEMBL4087344 IC50 > 1000.0 nM -
CHEMBL4103488 IC50 > 1000.0 nM -
CHEMBL4079230 IC50 > 1000.0 nM -
CHEMBL4059730 IC50 > 1000.0 nM -
CHEMBL4094045 IC50 > 1000.0 nM -