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Assay Detail

CHEMBL2216290

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

Binding
Inhibition of N-terminal 6His-tagged full length human recombinant STK33 using myelin basic protein as substrate incubated for 15 mins before initiation of kinase reaction measured after 1 hr by 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 33 (CHEMBL6005)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.
Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA, Stern AM, Schreiber SL, Munoz B.
ACS Med Chem Lett (2012) 3 : 1034 -1038
PubMed 23256033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.57 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2203524 1 8.15
CHEMBL2203525 1 7.96
CHEMBL2204239 1 7.85
CHEMBL2203528 1 7.12
CHEMBL2204241 1 7.11
CHEMBL2204238 1 6.96
CHEMBL2203530 1 6.82
CHEMBL2204235 1 6.80
CHEMBL1992679 1 6.77
CHEMBL2204237 1 6.60
CHEMBL2204240 1 6.57
CHEMBL1543343 1 6.55
CHEMBL2203531 1 6.52
CHEMBL2203526 1 6.42
CHEMBL2204236 1 6.39
CHEMBL2203527 1 6.28
CHEMBL2203529 1 6.24
CHEMBL2203532 1 6.01
CHEMBL2204234 1 5.80
CHEMBL2203536 1 5.80
CHEMBL2204233 1 5.80
CHEMBL2204232 1 5.40
CHEMBL2204231 1 5.14
CHEMBL2204230 1 -
CHEMBL2203533 1 -
CHEMBL2203534 1 -
CHEMBL2203535 1 -
CHEMBL2204228 1 -
CHEMBL2204229 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2203524 IC50 = 7.0 nM 8.15
CHEMBL2203525 IC50 = 11.0 nM 7.96
CHEMBL2204239 IC50 = 14.0 nM 7.85
CHEMBL2203528 IC50 = 76.0 nM 7.12
CHEMBL2204241 IC50 = 78.0 nM 7.11
CHEMBL2204238 IC50 = 110.0 nM 6.96
CHEMBL2203530 IC50 = 150.0 nM 6.82
CHEMBL2204235 IC50 = 160.0 nM 6.80
CHEMBL1992679 IC50 = 170.0 nM 6.77
CHEMBL2204237 IC50 = 250.0 nM 6.60
CHEMBL2204240 IC50 = 270.0 nM 6.57
CHEMBL1543343 IC50 = 280.0 nM 6.55
CHEMBL2203531 IC50 = 300.0 nM 6.52
CHEMBL2203526 IC50 = 380.0 nM 6.42
CHEMBL2204236 IC50 = 410.0 nM 6.39
CHEMBL2203527 IC50 = 530.0 nM 6.28
CHEMBL2203529 IC50 = 580.0 nM 6.24
CHEMBL2203532 IC50 = 980.0 nM 6.01
CHEMBL2204234 IC50 = 1600.0 nM 5.80
CHEMBL2203536 IC50 = 1600.0 nM 5.80
CHEMBL2204233 IC50 = 1600.0 nM 5.80
CHEMBL2204232 IC50 = 4000.0 nM 5.40
CHEMBL2204231 IC50 = 7300.0 nM 5.14
CHEMBL2204230 IC50 > 10000.0 nM -
CHEMBL2203533 IC50 > 10000.0 nM -
CHEMBL2203534 IC50 > 10000.0 nM -
CHEMBL2203535 IC50 > 10000.0 nM -
CHEMBL2204228 IC50 > 10000.0 nM -
CHEMBL2204229 IC50 > 10000.0 nM -