Assay Detail

CHEMBL4199987

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Functional

Antiproliferative activity against human A2058 cells harboring BRAF V600E/D mutant measured after 4 days

ChEMBL ↗

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Target

A2058 (CHEMBL613503) ↗

Open DB target context

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A2058 (CHEMBL613503) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target A2058

CHEMBL613503

Anchored from Assay target.

Protein identity A2058

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
Cell Type	A2058
Confidence	1 — Organism
Curated By	Intermediate

Target

A2058 (CHEMBL613503) ↗

Type	CELL-LINE
Organism	Homo sapiens

Publication

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA.
ACS Med Chem Lett (2018) 9 : 761 -767
PubMed 30034615 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.43	6.43

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4213970	MK-8353	1.0	1	6.43

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4213970	MK-8353	IC50	=	371.0	nM	6.43