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Assay Detail

CHEMBL5258809

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

Binding
Inhibition of human SOS1/GST-tagged KRAS G12C mutant (unknown origin) protein-protein interaction expressed in Escherichia coli BL21(DE3) incubated for 30 mins by NMR analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

SOS1-KRAS (CHEMBL5465393)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of quinazoline SOS1 inhibitors.
Jiang H, Fan Y, Wang X, Wang J, Yang H, Fan W, Tang C.
Bioorg Med Chem Lett (2023) 88 : 129265 -129265
PubMed 37011767 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.04 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519023 1 8.40
CHEMBL4535474 BAY-293 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519023 IC50 = 4.0 nM 8.40
CHEMBL4535474 BAY-293 IC50 = 21.0 nM 7.68