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Assay Detail

CHEMBL5516730

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

Binding
Inhibition of N-terminal His6-tagged rat RSK1 expressed in baculovirus infected Sf21 cells 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 Rattus norvegicus
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosomal protein S6 kinase alpha-1 (CHEMBL5528)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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