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Assay Detail

CHEMBL4742450

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

Binding
Inhibition of haspin in human SW620 cells assessed as reduction in IFNgamma-induced H3T3 phosphorylation pre-incubated for 1 hr before IFNgamma stimulation for 3 hrs by Western blot analysis
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SW-620
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase haspin (CHEMBL1075163)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Condensed tricyclic compounds as protein kinase inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
INH 8 - -
IC50 1 8.80 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4791276 1 8.80
CHEMBL4779550 1 -
CHEMBL4790936 1 -
CHEMBL4777501 1 -
CHEMBL4778840 1 -
CHEMBL4782696 1 -
CHEMBL4781993 1 -
CHEMBL4793477 1 -
CHEMBL4782203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4791276 IC50 = 1.6 nM 8.80
CHEMBL4779550 INH < 500.0 nM -
CHEMBL4790936 INH < 500.0 nM -
CHEMBL4777501 INH < 500.0 nM -
CHEMBL4778840 INH < 500.0 nM -
CHEMBL4782696 INH < 500.0 nM -
CHEMBL4781993 INH < 500.0 nM -
CHEMBL4793477 INH < 500.0 nM -
CHEMBL4782203 INH < 500.0 nM -