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Assay Detail

CHEMBL911979

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

Binding
Inhibition of GST-MLK3 expressed in baculovirus
28
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mitogen-activated protein kinase kinase kinase 11 (CHEMBL2708)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.
Hudkins RL, Johnson NW, Angeles TS, Gessner GW, Mallamo JP.
J Med Chem (2007) 50 : 433 -441
PubMed 17266195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.96 7.92
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386636 1 7.92
CHEMBL416056 1 7.89
CHEMBL374581 1 7.66
CHEMBL221536 1 7.58
CHEMBL357490 1 7.40
CHEMBL16958 STAUROSPORINONE 1 7.31
CHEMBL126545 1 7.24
CHEMBL148471 1 7.06
CHEMBL384914 1 6.96
CHEMBL220497 1 6.80
CHEMBL220799 1 6.77
CHEMBL426719 1 6.57
CHEMBL375220 1 6.56
CHEMBL332575 1 6.52
CHEMBL375085 1 6.14
CHEMBL374639 1 5.96
CHEMBL17031 1 5.92
CHEMBL374722 1 -
CHEMBL220961 1 -
CHEMBL374353 1 -
CHEMBL201931 1 -
CHEMBL202426 1 -
CHEMBL278969 1 -
CHEMBL219159 1 -
CHEMBL375093 1 -
CHEMBL222068 1 -
CHEMBL375139 1 -
CHEMBL438054 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386636 IC50 = 12.0 nM 7.92
CHEMBL416056 IC50 = 13.0 nM 7.89
CHEMBL374581 IC50 = 22.0 nM 7.66
CHEMBL221536 IC50 = 26.0 nM 7.58
CHEMBL357490 IC50 = 40.0 nM 7.40
CHEMBL16958 STAUROSPORINONE IC50 = 49.0 nM 7.31
CHEMBL126545 IC50 = 58.0 nM 7.24
CHEMBL148471 IC50 = 87.0 nM 7.06
CHEMBL384914 IC50 = 110.0 nM 6.96
CHEMBL220497 IC50 = 157.0 nM 6.80
CHEMBL220799 IC50 = 171.0 nM 6.77
CHEMBL426719 IC50 = 270.0 nM 6.57
CHEMBL375220 IC50 = 277.0 nM 6.56
CHEMBL332575 IC50 = 300.0 nM 6.52
CHEMBL375085 IC50 = 724.0 nM 6.14
CHEMBL374639 IC50 = 1106.0 nM 5.96
CHEMBL17031 IC50 = 1200.0 nM 5.92
CHEMBL374722 Activity - -
CHEMBL220961 IC50 > 300.0 nM -
CHEMBL374353 Activity - -
CHEMBL201931 IC50 > 1000.0 nM -
CHEMBL202426 IC50 > 1000.0 nM -
CHEMBL278969 IC50 > 10000.0 nM -
CHEMBL219159 IC50 > 300.0 nM -
CHEMBL375093 IC50 > 300.0 nM -
CHEMBL222068 IC50 > 10000.0 nM -
CHEMBL375139 IC50 > 300.0 nM -
CHEMBL438054 IC50 > 300.0 nM -