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Assay Detail

CHEMBL944209

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

Functional
Abrogation of camptothecin induced cell cycle arrest at G2/M phase in human HT29 cells
58
Total Activities
58
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

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD.
Bioorg Med Chem Lett (2008) 18 : 4242 -4248
PubMed 18547806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 58 6.43 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518661 1 7.77
CHEMBL487273 1 7.70
CHEMBL517553 1 7.70
CHEMBL516784 1 7.52
CHEMBL513377 1 7.40
CHEMBL470288 1 7.40
CHEMBL488044 1 7.22
CHEMBL513191 1 7.16
CHEMBL459631 1 7.10
CHEMBL469481 1 7.10
CHEMBL488287 1 7.05
CHEMBL471096 1 6.96
CHEMBL486234 1 6.89
CHEMBL469686 1 6.77
CHEMBL520902 1 6.70
CHEMBL507700 1 6.57
CHEMBL488230 1 6.52
CHEMBL527881 1 6.50
CHEMBL488231 1 6.47
CHEMBL459650 1 6.24
CHEMBL488835 1 6.21
CHEMBL487437 1 6.04
CHEMBL508982 1 6.02
CHEMBL518777 1 5.96
CHEMBL459428 1 5.92
CHEMBL504542 1 5.75
CHEMBL519226 1 5.72
CHEMBL471094 1 5.68
CHEMBL488039 1 5.66
CHEMBL486233 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518661 EC50 = 17.0 nM 7.77
CHEMBL487273 EC50 = 20.0 nM 7.70
CHEMBL517553 EC50 = 20.0 nM 7.70
CHEMBL516784 EC50 = 30.0 nM 7.52
CHEMBL513377 EC50 = 40.0 nM 7.40
CHEMBL470288 EC50 = 40.0 nM 7.40
CHEMBL488044 EC50 = 60.0 nM 7.22
CHEMBL513191 EC50 = 70.0 nM 7.16
CHEMBL459631 EC50 = 80.0 nM 7.10
CHEMBL469481 EC50 = 80.0 nM 7.10
CHEMBL488287 EC50 = 90.0 nM 7.05
CHEMBL471096 EC50 = 110.0 nM 6.96
CHEMBL486234 EC50 = 130.0 nM 6.89
CHEMBL469686 EC50 = 170.0 nM 6.77
CHEMBL520902 EC50 = 200.0 nM 6.70
CHEMBL507700 EC50 = 270.0 nM 6.57
CHEMBL488230 EC50 = 300.0 nM 6.52
CHEMBL527881 EC50 = 320.0 nM 6.50
CHEMBL488231 EC50 = 340.0 nM 6.47
CHEMBL459650 EC50 = 580.0 nM 6.24
CHEMBL488835 EC50 = 610.0 nM 6.21
CHEMBL487437 EC50 = 920.0 nM 6.04
CHEMBL508982 EC50 = 960.0 nM 6.02
CHEMBL518777 EC50 = 1100.0 nM 5.96
CHEMBL459428 EC50 = 1200.0 nM 5.92
CHEMBL504542 EC50 = 1800.0 nM 5.75
CHEMBL519226 EC50 = 1900.0 nM 5.72
CHEMBL471094 EC50 = 2100.0 nM 5.68
CHEMBL488039 EC50 = 2200.0 nM 5.66
CHEMBL486233 EC50 = 2300.0 nM 5.64
CHEMBL471549 EC50 = 2600.0 nM 5.58
CHEMBL519248 EC50 = 3200.0 nM 5.50
CHEMBL459651 EC50 = 4100.0 nM 5.39
CHEMBL487622 EC50 = 4300.0 nM 5.37
CHEMBL471095 EC50 = 6200.0 nM 5.21
CHEMBL470289 EC50 = 8100.0 nM 5.09
CHEMBL459442 EC50 - -
CHEMBL516615 EC50 - -
CHEMBL461914 EC50 - -
CHEMBL512706 EC50 - -
CHEMBL520734 EC50 < 9.0 nM -
CHEMBL471548 EC50 - -
CHEMBL488238 EC50 - -
CHEMBL452020 EC50 > 12500.0 nM -
CHEMBL460889 EC50 > 12500.0 nM -
CHEMBL460888 EC50 > 12500.0 nM -
CHEMBL511138 EC50 > 13000.0 nM -
CHEMBL519913 EC50 < 8.0 nM -
CHEMBL452021 EC50 > 12500.0 nM -
CHEMBL461294 EC50 > 12500.0 nM -