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Assay Detail

CHEMBL4003771

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

Binding
Inhibition of human CLK4 using YRRAAVPPSPSLSRHSSPHQS(p)EDEEE as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method
19
Total Activities
17
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

Dual specificity protein kinase CLK4 (CHEMBL4203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.
Shi Y, Park J, Lagisetti C, Zhou W, Sambucetti LC, Webb TR.
Bioorg Med Chem Lett (2017) 27 : 406 -412
PubMed 28049589 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.03 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078898 2 7.60
CHEMBL4104657 1 7.55
CHEMBL4094492 2 7.52
CHEMBL4067013 1 7.51
CHEMBL4066861 1 7.30
CHEMBL4064123 1 7.21
CHEMBL4073318 1 7.16
CHEMBL4102101 1 7.11
CHEMBL4088144 1 7.07
CHEMBL4091876 1 6.99
CHEMBL367625 1 6.98
CHEMBL4082309 1 6.91
CHEMBL4084116 1 6.52
CHEMBL4080283 1 6.30
CHEMBL4104505 1 6.20
CHEMBL4100324 1 6.19
CHEMBL1532768 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078898 IC50 = 25.0 nM 7.60
CHEMBL4104657 IC50 = 28.0 nM 7.55
CHEMBL4094492 IC50 = 30.0 nM 7.52
CHEMBL4067013 IC50 = 31.0 nM 7.51
CHEMBL4066861 IC50 = 50.0 nM 7.30
CHEMBL4078898 IC50 = 54.0 nM 7.27
CHEMBL4064123 IC50 = 61.0 nM 7.21
CHEMBL4094492 IC50 = 64.0 nM 7.19
CHEMBL4073318 IC50 = 70.0 nM 7.16
CHEMBL4102101 IC50 = 77.0 nM 7.11
CHEMBL4088144 IC50 = 86.0 nM 7.07
CHEMBL4091876 IC50 = 102.0 nM 6.99
CHEMBL367625 IC50 = 104.0 nM 6.98
CHEMBL4082309 IC50 = 124.0 nM 6.91
CHEMBL4084116 IC50 = 299.0 nM 6.52
CHEMBL4080283 IC50 = 498.0 nM 6.30
CHEMBL4104505 IC50 = 634.0 nM 6.20
CHEMBL4100324 IC50 = 648.0 nM 6.19
CHEMBL1532768 IC50 > 1000.0 nM -