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Assay Detail

CHEMBL950060

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

Binding
Inhibition of recombinant Chk1
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Hasvold LA, Wang L, Przytulinska M, Xiao Z, Chen Z, Gu WZ, Merta PJ, Xue J, Kovar P, Zhang H, Park C, Sowin TJ, Rosenberg SH, Lin NH.
Bioorg Med Chem Lett (2008) 18 : 2311 -2315
PubMed 18358720 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.31 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270181 1 9.24
CHEMBL404189 1 9.22
CHEMBL256193 1 9.15
CHEMBL410195 1 9.05
CHEMBL256192 1 9.01
CHEMBL270417 1 8.72
CHEMBL255183 1 8.59
CHEMBL404152 1 8.51
CHEMBL403192 1 8.47
CHEMBL257067 1 8.46
CHEMBL257703 1 8.40
CHEMBL404479 1 8.40
CHEMBL272347 1 8.32
CHEMBL257512 1 8.17
CHEMBL272711 1 8.10
CHEMBL411098 1 8.09
CHEMBL257317 1 8.05
CHEMBL389816 1 8.00
CHEMBL271727 1 7.95
CHEMBL404498 1 7.81
CHEMBL427720 1 7.79
CHEMBL255816 1 7.66
CHEMBL404021 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270181 IC50 = 0.58 nM 9.24
CHEMBL404189 IC50 = 0.6 nM 9.22
CHEMBL256193 IC50 = 0.7 nM 9.15
CHEMBL410195 IC50 = 0.9 nM 9.05
CHEMBL256192 IC50 = 0.98 nM 9.01
CHEMBL270417 IC50 = 1.9 nM 8.72
CHEMBL255183 IC50 = 2.6 nM 8.59
CHEMBL404152 IC50 = 3.1 nM 8.51
CHEMBL403192 IC50 = 3.4 nM 8.47
CHEMBL257067 IC50 = 3.5 nM 8.46
CHEMBL257703 IC50 = 4.0 nM 8.40
CHEMBL404479 IC50 = 4.0 nM 8.40
CHEMBL272347 IC50 = 4.8 nM 8.32
CHEMBL257512 IC50 = 6.8 nM 8.17
CHEMBL272711 IC50 = 7.9 nM 8.10
CHEMBL411098 IC50 = 8.1 nM 8.09
CHEMBL257317 IC50 = 9.0 nM 8.05
CHEMBL389816 IC50 = 10.0 nM 8.00
CHEMBL271727 IC50 = 11.2 nM 7.95
CHEMBL404498 IC50 = 15.5 nM 7.81
CHEMBL427720 IC50 = 16.2 nM 7.79
CHEMBL255816 IC50 = 22.0 nM 7.66
CHEMBL404021 IC50 = 1050.0 nM 5.98