Assay Detail

CHEMBL4012783

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Binding

Stimulation of BRAF-CRAF dimerization in human HCT116 cells by luciferase complementation assay

ChEMBL ↗

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Target

BRAF/CRAF (CHEMBL4106189) ↗

Open DB target context

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BRAF/CRAF (CHEMBL4106189) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target BRAF/CRAF

CHEMBL4106189

Anchored from Assay target.

Protein identity BRAF/CRAF

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	7 — Homologous single protein target
Curated By	Autocuration

Target

BRAF/CRAF (CHEMBL4106189) ↗

Type	PROTEIN COMPLEX
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
EC50	2	6.16	6.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1229517	VEMURAFENIB	4.0	1	6.22
CHEMBL3962812	—	—	1	6.10

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1229517	VEMURAFENIB	EC50	=	601.0	nM	6.22
CHEMBL3962812	—	EC50	=	796.0	nM	6.10