Assay Detail

CHEMBL1769336

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

Functional

Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

THP-1 (CHEMBL614245) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

THP-1 (CHEMBL614245) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target THP-1

CHEMBL614245

Anchored from Assay target.

Protein identity THP-1

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	THP-1
Confidence	1 — Organism
Curated By	Autocuration

Target

THP-1 (CHEMBL614245) ↗

Type	CELL-LINE
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
IC50	2	7.47	7.60

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1090089	PAMAPIMOD	2.0	1	7.60
CHEMBL1230122	R-1487	1.0	1	7.33

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1090089	PAMAPIMOD	IC50	=	25.0	nM	7.60
CHEMBL1230122	R-1487	IC50	=	47.0	nM	7.33