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Assay Detail

CHEMBL3536065

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

Binding
Inhibition of B-raf V600E mutant in human COLO205 cells assessed as reduction of ERK1/ERK2 phosphorylation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COLO 205
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.
Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH.
Drug Metab Dispos (2012) 40 : 919 -927
PubMed 22315332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.74 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2146883 COBIMETINIB 4.0 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2146883 COBIMETINIB IC50 = 1.8 nM 8.74