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Assay Detail

CHEMBL5107176

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

Binding
Inhibition of SOS1 in human DLD-1 cells assessed as reduction in ERK phosphorylation incubated for 1 hr by fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type DLD-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Son of sevenless homolog 1 (CHEMBL2079846)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Orally Bioavailable SOS1 Inhibitors for Suppressing KRAS-Driven Carcinoma.
He H, Zhang Y, Xu J, Li Y, Fang H, Liu Y, Zhang S.
J Med Chem (2022) 65 : 13158 -13171
PubMed 36173339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.50 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5171547 1 8.00
CHEMBL5184087 1 7.96
CHEMBL5184590 1 7.89
CHEMBL5201901 1 7.89
CHEMBL5196432 1 7.80
CHEMBL5209105 1 7.72
CHEMBL5195849 1 7.54
CHEMBL5201816 1 7.52
CHEMBL5185398 1 7.47
CHEMBL5203150 1 7.47
CHEMBL5183723 1 7.40
CHEMBL5170314 1 7.31
CHEMBL5185573 1 7.29
CHEMBL5193498 1 7.28
CHEMBL5208418 1 7.16
CHEMBL5183879 1 7.12
CHEMBL5191638 1 7.11
CHEMBL5181797 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5171547 IC50 = 10.0 nM 8.00
CHEMBL5184087 IC50 = 11.0 nM 7.96
CHEMBL5184590 IC50 = 13.0 nM 7.89
CHEMBL5201901 IC50 = 13.0 nM 7.89
CHEMBL5196432 IC50 = 16.0 nM 7.80
CHEMBL5209105 IC50 = 19.0 nM 7.72
CHEMBL5195849 IC50 = 29.0 nM 7.54
CHEMBL5201816 IC50 = 30.0 nM 7.52
CHEMBL5185398 IC50 = 34.0 nM 7.47
CHEMBL5203150 IC50 = 34.0 nM 7.47
CHEMBL5183723 IC50 = 40.0 nM 7.40
CHEMBL5170314 IC50 = 49.0 nM 7.31
CHEMBL5185573 IC50 = 51.0 nM 7.29
CHEMBL5193498 IC50 = 53.0 nM 7.28
CHEMBL5208418 IC50 = 70.0 nM 7.16
CHEMBL5183879 IC50 = 75.0 nM 7.12
CHEMBL5191638 IC50 = 78.0 nM 7.11
CHEMBL5181797 IC50 = 88.0 nM 7.06