Assay Detail

CHEMBL4012781

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Binding

Inhibition of full-length BRAF (unknown origin)

ChEMBL ↗

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Target

Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗

Open DB target context

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Serine/threonine-protein kinase B-raf (CHEMBL5145) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Serine/threonine-protein kinase B-raf

CHEMBL5145

Anchored from Assay target.

Protein identity Serine/threonine-protein kinase B-raf

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.

Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S.
J Med Chem (2017) 60 : 4869 -4881
PubMed 28557458 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.40	9.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3962812	—	—	1	9.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3962812	—	IC50	=	0.4	nM	9.40