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Assay Detail

CHEMBL5251827

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

Binding
PROTAC activity at VHL/SOS1 in human NCI-H441 cells harboring KRAS G12V mutant assessed as induction of SOS1 degradation incubated for 24 hrs by Immunoblot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NCI-H441
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

von Hippel-Lindau disease tumor suppressor/SOS1 (CHEMBL5169070)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers.
Zhou Z, Zhou G, Zhou C, Fan Z, Cui R, Li Y, Li R, Gu Y, Li H, Ge Z, Cai X, Jiang B, Wang D, Zheng M, Xu T, Zhang S.
J Med Chem (2023) 66 : 4197 -4214
PubMed 36897932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.07 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5287923 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5287923 EC50 = 8.41 nM 8.07