Assay Detail

CHEMBL1769337

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Functional

Inhibition of LPS-induced IL-6 production in po dosed rat serum administered 30 mins before LPS challenge measured after 1.5 hrs by ELISA

ChEMBL ↗

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Target

Rattus norvegicus (CHEMBL376) ↗

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Rattus norvegicus (CHEMBL376) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Rattus norvegicus

CHEMBL376

Anchored from Assay target.

Protein identity Rattus norvegicus

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	Functional
Organism	Rattus norvegicus
Tissue	Serum
Confidence	1 — Organism
Curated By	Autocuration

Target

Rattus norvegicus (CHEMBL376) ↗

Type	ORGANISM
Organism	Rattus norvegicus

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
ED50	2	-	-
EC50	2	7.65	8.00

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1230122	R-1487	1.0	2	8.00
CHEMBL1090089	PAMAPIMOD	2.0	2	7.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1230122	R-1487	EC50	=	10.0	nM	8.00
CHEMBL1090089	PAMAPIMOD	EC50	=	50.0	nM	7.30
CHEMBL1230122	R-1487	ED50	=	0.4	mg.kg-1	-
CHEMBL1090089	PAMAPIMOD	ED50	=	0.1	mg.kg-1	-