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Assay Detail

CHEMBL868464

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

Functional
Inhibition of cell cycle arrest in H1299 cells at G2 phase in presence of 500 nM doxorubicin by FACS assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1299
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H1299 (CHEMBL612255)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Li G, Hasvold LA, Tao ZF, Wang GT, Gwaltney SL, Patel J, Kovar P, Credo RB, Chen Z, Zhang H, Park C, Sham HL, Sowin T, Rosenberg SH, Lin NH.
Bioorg Med Chem Lett (2006) 16 : 2293 -2298
PubMed 16446090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.18 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL202635 1 6.85
CHEMBL206812 1 6.24
CHEMBL205449 1 5.84
CHEMBL208332 1 5.77
CHEMBL206997 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL202635 EC50 = 140.0 nM 6.85
CHEMBL206812 EC50 = 580.0 nM 6.24
CHEMBL205449 EC50 = 1450.0 nM 5.84
CHEMBL208332 EC50 = 1710.0 nM 5.77
CHEMBL206997 EC50 > 10000.0 nM -