Assay Detail

CHEMBL5705996

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Binding

Inhibition of Raf-MEK-ERK pathway in human COLO 205 cells harboring B-Raf V600E mutant assessed as inhibition of ERK phosphorylation incubated for 1 hrs by immunoblotting based luminometer analysis

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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
Organism	Homo sapiens
Cell Type	COLO 205
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, Bremer R, Gillette S, Kong J, Haass NK, Sproesser K, Li L, Smalley KS, Fong D, Zhu YL, Marimuthu A, Nguyen H, Lam B, Liu J, Cheung I, Rice J, Suzuki Y, Luu C, Settachatgul C, Shellooe R, Cantwell J, Kim SH, Schlessinger J, Zhang KY, West BL, Powell B, Habets G, Zhang C, Ibrahim PN, Hirth P, Artis DR, Herlyn M, Bollag G.
Proc Natl Acad Sci U S A (2008) 105 : 3041 -3046
PubMed 18287029 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.85	7.85

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000756
EFO_TERM	EFO_TERM	-	—	melanoma

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1230020	PLX-4720	—	1	7.85
CHEMBL507361	MIRDAMETINIB	2.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1230020	PLX-4720	IC50	=	14.0	nM	7.85
CHEMBL507361	MIRDAMETINIB	IC50	<	2.0	nM	-