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Assay Detail

CHEMBL4344002

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

Binding
Displacement of [3H]-cGAMP from full length STING HAQ mutant in human THP1 cells by filtration binding assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Stimulator of interferon genes protein (CHEMBL4523377)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.
Zhang H, You QD, Xu XL.
J Med Chem (2020) 63 : 3785 -3816
PubMed 31820978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.34 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465286 1 8.92
CHEMBL4456045 1 8.77
CHEMBL4568160 1 7.93
CHEMBL4553220 1 7.67
CHEMBL4476354 1 7.61
CHEMBL4468545 1 6.28
CHEMBL4562620 1 6.22
CHEMBL4575454 1 6.05
CHEMBL4436937 1 5.86
CHEMBL4434776 1 5.76
CHEMBL4467434 1 5.58
CHEMBL4570444 1 5.56
CHEMBL4528146 1 5.39
CHEMBL4475752 1 5.26
CHEMBL4574326 1 5.22
CHEMBL4440309 1 5.02
CHEMBL4436665 1 4.75
CHEMBL4556279 1 -
CHEMBL4525655 1 -
CHEMBL4521873 1 -
CHEMBL4474321 1 -
CHEMBL4459212 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465286 EC50 = 1.2 nM 8.92
CHEMBL4456045 EC50 = 1.7 nM 8.77
CHEMBL4568160 EC50 = 11.7 nM 7.93
CHEMBL4553220 EC50 = 21.5 nM 7.67
CHEMBL4476354 EC50 = 24.6 nM 7.61
CHEMBL4468545 EC50 = 531.0 nM 6.28
CHEMBL4562620 EC50 = 599.0 nM 6.22
CHEMBL4575454 EC50 = 894.0 nM 6.05
CHEMBL4436937 EC50 = 1375.0 nM 5.86
CHEMBL4434776 EC50 = 1720.0 nM 5.76
CHEMBL4467434 EC50 = 2636.0 nM 5.58
CHEMBL4570444 EC50 = 2735.0 nM 5.56
CHEMBL4528146 EC50 = 4073.0 nM 5.39
CHEMBL4475752 EC50 = 5547.0 nM 5.26
CHEMBL4574326 EC50 = 5990.0 nM 5.22
CHEMBL4440309 EC50 = 9587.0 nM 5.02
CHEMBL4436665 EC50 = 17840.0 nM 4.75
CHEMBL4556279 EC50 < 1.0 nM -
CHEMBL4525655 EC50 < 1.0 nM -
CHEMBL4521873 EC50 < 1.0 nM -
CHEMBL4474321 EC50 < 1.0 nM -
CHEMBL4459212 EC50 < 1.0 nM -