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Assay Detail

CHEMBL4723758

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

Binding
Binding affinity to C-terminal nano-luciferase tagged STK17B (unknown origin) expressed in HEK293 cells incubated for 2 hrs by nano-BRET assay based cellular target engagement assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase 17B (CHEMBL3980)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
Picado A,Chaikuad A,Wells CI,Shrestha S,Zuercher WJ,Pickett JE,Kwarcinski FE,Sinha P,de Silva CS,Zutshi R,Liu S,Kannan N,Knapp S,Drewry DH,Willson TM
J Med Chem (2020) 63 : 14626 -14646
PubMed 33215924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.20 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4794509 1 6.92
CHEMBL4752776 1 6.72
CHEMBL1836719 1 6.68
CHEMBL4755086 1 6.51
CHEMBL4788024 1 6.47
CHEMBL4753625 1 6.42
CHEMBL4788686 1 6.30
CHEMBL4789685 1 6.30
CHEMBL4754748 1 6.28
CHEMBL4739879 1 6.28
CHEMBL4748440 1 6.26
CHEMBL4792541 1 6.19
CHEMBL1836714 1 6.17
CHEMBL4763132 1 6.16
CHEMBL4753926 1 6.14
CHEMBL4748561 1 6.09
CHEMBL4783516 1 6.06
CHEMBL4745018 1 6.01
CHEMBL4788886 1 5.92
CHEMBL4760126 1 5.82
CHEMBL4752999 1 5.77
CHEMBL4781408 1 5.54
CHEMBL1836717 1 5.50
CHEMBL4756902 1 -
CHEMBL4763392 1 -
CHEMBL4740090 1 -
CHEMBL4782453 1 -
CHEMBL4761540 1 -
CHEMBL1836637 1 -
CHEMBL4745289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4794509 IC50 = 120.0 nM 6.92
CHEMBL4752776 IC50 = 190.0 nM 6.72
CHEMBL1836719 IC50 = 210.0 nM 6.68
CHEMBL4755086 IC50 = 310.0 nM 6.51
CHEMBL4788024 IC50 = 340.0 nM 6.47
CHEMBL4753625 IC50 = 380.0 nM 6.42
CHEMBL4788686 IC50 = 500.0 nM 6.30
CHEMBL4789685 IC50 = 500.0 nM 6.30
CHEMBL4754748 IC50 = 530.0 nM 6.28
CHEMBL4739879 IC50 = 530.0 nM 6.28
CHEMBL4748440 IC50 = 550.0 nM 6.26
CHEMBL4792541 IC50 = 650.0 nM 6.19
CHEMBL1836714 IC50 = 680.0 nM 6.17
CHEMBL4763132 IC50 = 700.0 nM 6.16
CHEMBL4753926 IC50 = 720.0 nM 6.14
CHEMBL4748561 IC50 = 820.0 nM 6.09
CHEMBL4783516 IC50 = 870.0 nM 6.06
CHEMBL4745018 IC50 = 980.0 nM 6.01
CHEMBL4788886 IC50 = 1200.0 nM 5.92
CHEMBL4760126 IC50 = 1500.0 nM 5.82
CHEMBL4752999 IC50 = 1700.0 nM 5.77
CHEMBL4781408 IC50 = 2900.0 nM 5.54
CHEMBL1836717 IC50 = 3200.0 nM 5.50
CHEMBL4799235 IC50 > 10000.0 nM -
CHEMBL4753500 IC50 > 10000.0 nM -
CHEMBL4793795 IC50 > 10000.0 nM -
CHEMBL4759004 IC50 > 10000.0 nM -
CHEMBL1836724 IC50 > 10000.0 nM -
CHEMBL4740604 IC50 > 10000.0 nM -
CHEMBL4747753 IC50 > 10000.0 nM -
CHEMBL4796519 IC50 > 10000.0 nM -
CHEMBL4794226 IC50 > 10000.0 nM -
CHEMBL4754574 IC50 > 10000.0 nM -
CHEMBL4763345 IC50 > 10000.0 nM -
CHEMBL4745289 IC50 > 10000.0 nM -
CHEMBL1836637 IC50 > 10000.0 nM -
CHEMBL4761540 IC50 > 10000.0 nM -
CHEMBL4782453 IC50 > 10000.0 nM -
CHEMBL4740090 IC50 > 10000.0 nM -
CHEMBL4763392 IC50 > 10000.0 nM -
CHEMBL4756902 IC50 > 10000.0 nM -