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Assay Detail

CHEMBL3370356

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

Binding
Inhibition of Chk1 (unknown origin) by luminescent ADP-Glo assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.
Song P, Peng P, Han M, Cao X, Ma X, Liu T, Zhou Y, Hu Y.
Bioorg Med Chem (2014) 22 : 4882 -4892
PubMed 25042558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.89 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330232 1 8.63
CHEMBL3330227 1 8.45
CHEMBL3330148 1 8.39
CHEMBL3330230 1 8.32
CHEMBL3330133 1 8.28
CHEMBL3330233 1 8.27
CHEMBL3330229 1 8.21
CHEMBL3330236 1 8.12
CHEMBL2041933 AZD-7762 1.0 1 8.10
CHEMBL3330234 1 8.01
CHEMBL3330135 1 8.00
CHEMBL3330136 1 7.85
CHEMBL3330231 1 7.81
CHEMBL3330132 1 7.81
CHEMBL3330235 1 7.63
CHEMBL3330237 1 7.61
CHEMBL3330228 1 7.39
CHEMBL3330134 1 7.32
CHEMBL3330138 1 6.93
CHEMBL3330141 1 6.75
CHEMBL3330145 1 -
CHEMBL3330144 1 -
CHEMBL3330143 1 -
CHEMBL3330142 1 -
CHEMBL3330140 1 -
CHEMBL3330139 1 -
CHEMBL3330137 1 -
CHEMBL3330146 1 -
CHEMBL3330147 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330232 IC50 = 2.33 nM 8.63
CHEMBL3330227 IC50 = 3.53 nM 8.45
CHEMBL3330148 IC50 = 4.05 nM 8.39
CHEMBL3330230 IC50 = 4.83 nM 8.32
CHEMBL3330133 IC50 = 5.22 nM 8.28
CHEMBL3330233 IC50 = 5.36 nM 8.27
CHEMBL3330229 IC50 = 6.23 nM 8.21
CHEMBL3330236 IC50 = 7.54 nM 8.12
CHEMBL2041933 AZD-7762 IC50 = 7.89 nM 8.10
CHEMBL3330234 IC50 = 9.84 nM 8.01
CHEMBL3330135 IC50 = 9.94 nM 8.00
CHEMBL3330136 IC50 = 14.02 nM 7.85
CHEMBL3330231 IC50 = 15.34 nM 7.81
CHEMBL3330132 IC50 = 15.6 nM 7.81
CHEMBL3330235 IC50 = 23.2 nM 7.63
CHEMBL3330237 IC50 = 24.73 nM 7.61
CHEMBL3330228 IC50 = 40.98 nM 7.39
CHEMBL3330134 IC50 = 47.5 nM 7.32
CHEMBL3330138 IC50 = 116.1 nM 6.93
CHEMBL3330141 IC50 = 177.8 nM 6.75
CHEMBL3330145 IC50 > 10000.0 nM -
CHEMBL3330144 IC50 > 10000.0 nM -
CHEMBL3330143 IC50 > 10000.0 nM -
CHEMBL3330142 IC50 > 10000.0 nM -
CHEMBL3330140 IC50 > 10000.0 nM -
CHEMBL3330139 IC50 > 10000.0 nM -
CHEMBL3330137 IC50 > 10000.0 nM -
CHEMBL3330146 IC50 > 10000.0 nM -
CHEMBL3330147 IC50 > 10000.0 nM -