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Assay Detail

CHEMBL3384714

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

Binding
Inhibition of BRAF (unknown origin)-mediated ERK phosphorylation by cell-based assay
17
Total Activities
17
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

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

Publication

Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Subramanian S, Costales A, Williams TE, Levine B, McBride CM, Poon D, Amiri P, Renhowe PA, Shafer CM, Stuart D, Verhagen J, Ramurthy S.
ACS Med Chem Lett (2014) 5 : 989 -992
PubMed 25221654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.05 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3335371 1 7.40
CHEMBL3335380 1 7.30
CHEMBL3335376 1 7.30
CHEMBL3335373 1 7.30
CHEMBL3335377 1 7.10
CHEMBL3335378 1 7.05
CHEMBL3335381 1 7.05
CHEMBL3335372 1 7.00
CHEMBL3335383 1 7.00
CHEMBL3335374 1 7.00
CHEMBL3335385 1 7.00
CHEMBL3335382 1 7.00
CHEMBL3335386 1 7.00
CHEMBL3335387 1 7.00
CHEMBL3335384 1 7.00
CHEMBL3335379 1 7.00
CHEMBL3335375 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3335371 EC50 = 40.0 nM 7.40
CHEMBL3335380 EC50 = 50.0 nM 7.30
CHEMBL3335376 EC50 = 50.0 nM 7.30
CHEMBL3335373 EC50 = 50.0 nM 7.30
CHEMBL3335377 EC50 = 80.0 nM 7.10
CHEMBL3335378 EC50 = 90.0 nM 7.05
CHEMBL3335381 EC50 = 90.0 nM 7.05
CHEMBL3335372 EC50 = 100.0 nM 7.00
CHEMBL3335383 EC50 = 100.0 nM 7.00
CHEMBL3335374 EC50 = 100.0 nM 7.00
CHEMBL3335385 EC50 = 100.0 nM 7.00
CHEMBL3335382 EC50 = 100.0 nM 7.00
CHEMBL3335386 EC50 = 100.0 nM 7.00
CHEMBL3335387 EC50 = 100.0 nM 7.00
CHEMBL3335384 EC50 = 100.0 nM 7.00
CHEMBL3335379 EC50 = 100.0 nM 7.00
CHEMBL3335375 EC50 = 400.0 nM 6.40