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Assay Detail

CHEMBL5529893

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

Functional
Antiproliferative activity against human SW837 cells incubated for 6 days in presence of 1 uM (2S,4R)-1-((S)-2-(5-((4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide by CCK8 assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SW837
Confidence 1 — Organism
Curated By Autocuration

Target

SW837 (CHEMBL1075596)
Type CELL-LINE
Organism Homo sapiens

Publication

A Potent SOS1 PROTAC Degrader with Synergistic Efficacy in Combination with KRAS<sup>G12C</sup> Inhibitor.
Lv Y, Yang Z, Chen Y, Ma X, Guo M, Zhang C, Jiang X, Wang C, Li Z, Tai Z, Wang X, Zhang S, Ma S, Qin C.
J Med Chem (2024) 67 : 2487 -2511
PubMed 38316747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4535757 SOTORASIB 4.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4535757 SOTORASIB IC50 = 3.0 nM 8.52