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Assay Detail

CHEMBL4014111

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

Binding
Inhibition of recombinant human CLK1 expressed in insect cells using ERMRPRKRQGSVRRRV peptide as substrate after 40 mins in presence of [gamma-33P]-ATP by scintillation counting
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

Dual specificity protein kinase CLK1 (CHEMBL4224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Sun QZ, Lin GF, Li LL, Jin XT, Huang LY, Zhang G, Yang W, Chen K, Xiang R, Chen C, Wei YQ, Lu GW, Yang SY.
J Med Chem (2017) 60 : 6337 -6352
PubMed 28692292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.10 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083249 1 8.70
CHEMBL4094600 1 8.22
CHEMBL4096379 1 8.15
CHEMBL408982 1 7.77
CHEMBL4072795 1 7.75
CHEMBL4067143 1 7.62
CHEMBL4060440 1 7.54
CHEMBL4093503 1 7.52
CHEMBL4104765 1 7.47
CHEMBL4088668 1 7.44
CHEMBL4069124 1 7.19
CHEMBL4104122 1 7.18
CHEMBL4079878 1 6.86
CHEMBL4064426 1 6.81
CHEMBL4086890 1 6.76
CHEMBL4100703 1 6.73
CHEMBL4081470 1 6.72
CHEMBL4063617 1 6.55
CHEMBL4092984 1 6.37
CHEMBL4072220 1 6.36
CHEMBL4082710 1 6.28
CHEMBL4104093 1 6.00
CHEMBL4078073 1 5.30
CHEMBL4059498 1 -
CHEMBL4102344 1 -
CHEMBL4074986 1 -
CHEMBL4101671 1 -
CHEMBL4085242 1 -
CHEMBL4086182 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083249 IC50 = 2.0 nM 8.70
CHEMBL4094600 IC50 = 6.0 nM 8.22
CHEMBL4096379 IC50 = 7.0 nM 8.15
CHEMBL408982 IC50 = 17.0 nM 7.77
CHEMBL4072795 IC50 = 18.0 nM 7.75
CHEMBL4067143 IC50 = 24.0 nM 7.62
CHEMBL4060440 IC50 = 29.0 nM 7.54
CHEMBL4093503 IC50 = 30.0 nM 7.52
CHEMBL4104765 IC50 = 34.0 nM 7.47
CHEMBL4088668 IC50 = 36.0 nM 7.44
CHEMBL4069124 IC50 = 64.0 nM 7.19
CHEMBL4104122 IC50 = 66.0 nM 7.18
CHEMBL4079878 IC50 = 139.0 nM 6.86
CHEMBL4064426 IC50 = 155.0 nM 6.81
CHEMBL4086890 IC50 = 173.0 nM 6.76
CHEMBL4100703 IC50 = 186.0 nM 6.73
CHEMBL4081470 IC50 = 189.0 nM 6.72
CHEMBL4063617 IC50 = 280.0 nM 6.55
CHEMBL4092984 IC50 = 430.0 nM 6.37
CHEMBL4072220 IC50 = 439.0 nM 6.36
CHEMBL4082710 IC50 = 529.0 nM 6.28
CHEMBL4104093 IC50 = 993.0 nM 6.00
CHEMBL4078073 IC50 = 4985.0 nM 5.30
CHEMBL4059498 IC50 > 10000.0 nM -
CHEMBL4102344 IC50 > 10000.0 nM -
CHEMBL4074986 IC50 > 10000.0 nM -
CHEMBL4101671 IC50 > 10000.0 nM -
CHEMBL4085242 IC50 > 10000.0 nM -
CHEMBL4086182 IC50 > 10000.0 nM -