Assay Detail

CHEMBL1769285

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Binding

Inhibition of RSK2

ChEMBL ↗

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Target

Ribosomal protein S6 kinase alpha-3 (CHEMBL2345) ↗

Open DB target context

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Ribosomal protein S6 kinase alpha-3 (CHEMBL2345) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Ribosomal protein S6 kinase alpha-3

CHEMBL2345

Anchored from Assay target.

Protein identity Ribosomal protein S6 kinase alpha-3

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Ribosomal protein S6 kinase alpha-3 (CHEMBL2345) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.

Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H.
J Med Chem (2011) 54 : 2255 -2265
PubMed 21375264 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	2	6.67	6.82

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1230122	R-1487	1.0	1	6.82
CHEMBL1090089	PAMAPIMOD	2.0	1	6.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1230122	R-1487	Kd	=	150.0	nM	6.82
CHEMBL1090089	PAMAPIMOD	Kd	=	300.0	nM	6.52