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Assay Detail

CHEMBL924432

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

Functional
Inhibition of camptothecin induced mitotic arrest in human NCI-H1299 cells after 18 hrs
28
Total Activities
28
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 Autocuration

Target

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

Publication

Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Garbaccio RM, Huang S, Tasber ES, Fraley ME, Yan Y, Munshi S, Ikuta M, Kuo L, Kreatsoulas C, Stirdivant S, Drakas B, Rickert K, Walsh ES, Hamilton KA, Buser CA, Hardwick J, Mao X, Beck SC, Abrams MT, Tao W, Lobell R, Sepp-Lorenzino L, Hartman GD.
Bioorg Med Chem Lett (2007) 17 : 6280 -6285
PubMed 17900896 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.71 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL249429 1 7.85
CHEMBL400350 1 7.36
CHEMBL249443 1 7.33
CHEMBL249224 1 7.19
CHEMBL249441 1 7.17
CHEMBL428409 1 7.10
CHEMBL400127 1 7.00
CHEMBL250035 1 6.89
CHEMBL249237 1 6.89
CHEMBL249044 1 6.85
CHEMBL249240 1 6.85
CHEMBL400323 1 6.82
CHEMBL401156 1 6.68
CHEMBL249241 1 6.64
CHEMBL249594 1 6.64
CHEMBL250459 1 6.57
CHEMBL249834 1 6.52
CHEMBL249595 1 6.51
CHEMBL250272 1 6.50
CHEMBL249632 1 6.43
CHEMBL250033 1 6.43
CHEMBL428580 1 6.02
CHEMBL248665 1 5.98
CHEMBL249236 1 5.96
CHEMBL250224 1 5.66
CHEMBL249238 1 -
CHEMBL250225 1 -
CHEMBL250222 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL249429 EC50 = 14.0 nM 7.85
CHEMBL400350 EC50 = 44.0 nM 7.36
CHEMBL249443 EC50 = 47.0 nM 7.33
CHEMBL249224 EC50 = 64.0 nM 7.19
CHEMBL249441 EC50 = 67.0 nM 7.17
CHEMBL428409 EC50 = 79.0 nM 7.10
CHEMBL400127 EC50 = 100.0 nM 7.00
CHEMBL250035 EC50 = 130.0 nM 6.89
CHEMBL249237 EC50 = 130.0 nM 6.89
CHEMBL249044 EC50 = 140.0 nM 6.85
CHEMBL249240 EC50 = 140.0 nM 6.85
CHEMBL400323 EC50 = 150.0 nM 6.82
CHEMBL401156 EC50 = 210.0 nM 6.68
CHEMBL249241 EC50 = 230.0 nM 6.64
CHEMBL249594 EC50 = 230.0 nM 6.64
CHEMBL250459 EC50 = 270.0 nM 6.57
CHEMBL249834 EC50 = 300.0 nM 6.52
CHEMBL249595 EC50 = 310.0 nM 6.51
CHEMBL250272 EC50 = 320.0 nM 6.50
CHEMBL249632 EC50 = 370.0 nM 6.43
CHEMBL250033 EC50 = 370.0 nM 6.43
CHEMBL428580 EC50 = 957.0 nM 6.02
CHEMBL248665 EC50 = 1050.0 nM 5.98
CHEMBL249236 EC50 = 1085.0 nM 5.96
CHEMBL250224 EC50 = 2200.0 nM 5.66
CHEMBL249238 EC50 > 10000.0 nM -
CHEMBL250225 EC50 > 10000.0 nM -
CHEMBL250222 EC50 - -