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Assay Detail

CHEMBL5109092

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

Binding
Inhibition of cGAS in human THP-1 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclic GMP-AMP synthase (CHEMBL4105728)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small molecules targeting cGAS-STING pathway for autoimmune disease.
Zhao J, Xiao R, Zeng R, He E, Zhang A.
Eur J Med Chem (2022) 238 : 114480 -114480
PubMed 35635952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.36 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174318 1 5.77
CHEMBL4448176 1 5.71
CHEMBL5081956 1 5.53
CHEMBL7568 QUINACRINE 4.0 1 5.16
CHEMBL1535 HYDROXYCHLOROQUINE 4.0 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174318 IC50 = 1700.0 nM 5.77
CHEMBL4448176 IC50 = 1960.0 nM 5.71
CHEMBL5081956 IC50 = 2950.0 nM 5.53
CHEMBL7568 QUINACRINE IC50 = 7000.0 nM 5.16
CHEMBL1535 HYDROXYCHLOROQUINE IC50 = 23000.0 nM 4.64