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Assay Detail

CHEMBL5516732

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

Binding
Inhibition of RSK3 (14 to 462 residues) (unknown origin) using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK peptide as substrate incubated for 10 mins in presence of [gamma-32p]ATP
1
Total Activities
1
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

Ribosomal protein S6 kinase alpha-2 (CHEMBL3906)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.
de Souza Gama FH, Dutra LA, Hawgood M, Dos Reis CV, Serafim RAM, Ferreira MA, Teodoro BVM, Takarada JE, Santiago AS, Balourdas DI, Nilsson AS, Urien B, Almeida VM, Gileadi C, Ramos PZ, Salmazo A, Vasconcelos SNS, Cunha MR, Mueller S, Knapp S, Massirer KB, Elkins JM, Gileadi O, Mascarello A, Lemmens BBLG, Guimarães CRW, Azevedo H, Couñago RM.
J Med Chem (2024) 67 : 8609 -8629
PubMed 38780468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573107 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573107 IC50 = 10.0 nM 8.00