Assay Detail

CHEMBL862333

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Functional

Inhibition of LPS-induced TNFalpha production in human PBMC

ChEMBL ↗

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Target

Mitogen-activated protein kinase 14 (CHEMBL260) ↗

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Primary target Mitogen-activated protein kinase 14

CHEMBL260

Anchored from Assay target.

Protein identity Mitogen-activated protein kinase 14

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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Expert

Target

Mitogen-activated protein kinase 14 (CHEMBL260) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.

Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S.
J Med Chem (2006) 49 : 1562 -1575
PubMed 16509574 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.40	6.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL203567	RO-3201195	1.0	1	6.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL203567	RO-3201195	IC50	=	400.0	nM	6.40