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Assay Detail

CHEMBL5540883

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

Binding
Inhibition of ERK phosphorylation in wild type human BJ cells incubated for 1 hr by HTRF analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BJ
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C, Martin ES, Miller N, Murphy EA, Timple N, Tyhonas JS, Vassar A, Wang TS, Williams R, Yuan D, Kania RS.
J Med Chem (2024) 67 : 1747 -1757
PubMed 38230963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.10 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5095099 EXARAFENIB 2.0 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5095099 EXARAFENIB EC50 = 7963.0 nM 5.10