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Assay Detail

CHEMBL2013772

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

Functional
Inhibition of cell cycle arrest in human HT-29 cells assessed as abrogation at G2/M checkpoint measuring phosphohistone-H3 level
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S.
Bioorg Med Chem Lett (2012) 22 : 2330 -2337
PubMed 22342147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 5.29 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012863 1 5.89
CHEMBL2012861 1 5.77
CHEMBL2012878 1 5.60
CHEMBL2012881 1 5.57
CHEMBL2012859 1 5.51
CHEMBL2012884 1 5.43
CHEMBL2012880 1 5.42
CHEMBL2012857 1 5.33
CHEMBL2012879 1 5.32
CHEMBL2012877 1 5.30
CHEMBL2012882 1 5.28
CHEMBL2012883 1 5.28
CHEMBL2012858 1 5.20
CHEMBL2012856 1 4.89
CHEMBL2012862 1 4.89
CHEMBL2012864 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012863 EC50 = 1300.0 nM 5.89
CHEMBL2012861 EC50 = 1700.0 nM 5.77
CHEMBL2012878 EC50 = 2500.0 nM 5.60
CHEMBL2012881 EC50 = 2700.0 nM 5.57
CHEMBL2012859 EC50 = 3100.0 nM 5.51
CHEMBL2012884 EC50 = 3700.0 nM 5.43
CHEMBL2012880 EC50 = 3800.0 nM 5.42
CHEMBL2012857 EC50 = 4700.0 nM 5.33
CHEMBL2012879 EC50 = 4800.0 nM 5.32
CHEMBL2012877 EC50 = 5000.0 nM 5.30
CHEMBL2012882 EC50 = 5300.0 nM 5.28
CHEMBL2012883 EC50 = 5300.0 nM 5.28
CHEMBL2012858 EC50 = 6300.0 nM 5.20
CHEMBL2012856 EC50 = 13000.0 nM 4.89
CHEMBL2012862 EC50 = 13000.0 nM 4.89
CHEMBL2012864 EC50 = 100000.0 nM 4.00