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Assay Detail

CHEMBL4629880

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

Binding
Inhibition of human MEK5 using ERK5 as substrate in presence of [gamma-33P]-ATP by hotspot kinase assay
4
Total Activities
4
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

Publication

Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity <i>in Vivo</i> Mouse Model.
Fromont C, Atzori A, Kaur D, Hashmi L, Greco G, Cabanillas A, Nguyen HV, Jones DH, Garzón M, Varela A, Stevenson B, Iacobini GP, Lenoir M, Rajesh S, Box C, Kumar J, Grant P, Novitskaya V, Morgan J, Sorrell FJ, Redondo C, Kramer A, Harris CJ, Leighton B, Vickers SP, Cheetham SC, Kenyon C, Grabowska AM, Overduin M, Berditchevski F, Weston CJ, Knapp S, Fischer PM, Butterworth S.
J Med Chem (2020) 63 : 6784 -6801
PubMed 32433887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.45 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635883 1 7.60
CHEMBL1835063 1 6.62
CHEMBL4640712 1 5.12
CHEMBL4648967 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635883 IC50 = 25.0 nM 7.60
CHEMBL1835063 IC50 = 240.0 nM 6.62
CHEMBL4640712 IC50 = 7680.0 nM 5.12
CHEMBL4648967 IC50 > 10000.0 nM -