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Assay Detail

CHEMBL4012780

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

Binding
Inhibition of CRAF in human Calu6 cells assessed as decrease in ERK phosphorylation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906)
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
EC50 1 7.00 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3962812 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3962812 EC50 = 100.0 nM 7.00