Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5162464

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

Binding
Agonist activity at STING HAQ variant in mouse BMDC cells assessed as increase in mouse INF-beta production incubated for 5 hrs by ELISA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BMDC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Stimulator of interferon genes protein (CHEMBL4523311)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Chang W, Altman MD, Lesburg CA, Perera SA, Piesvaux JA, Schroeder GK, Wyss DF, Cemerski S, Chen Y, DiNunzio E, Haidle AM, Ho T, Kariv I, Knemeyer I, Kopinja JE, Lacey BM, Laskey J, Lim J, Long BJ, Ma Y, Maddess ML, Pan BS, Presland JP, Spooner E, Steinhuebel D, Truong Q, Zhang Z, Fu J, Addona GH, Northrup AB, Parmee E, Tata JR, Bennett DJ, Cumming JN, Siu T, Trotter BW.
J Med Chem (2022) 65 : 5675 -5689
PubMed 35332774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 4.93 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188233 1 6.09
CHEMBL5185127 1 5.81
CHEMBL5197904 1 5.49
CHEMBL5093161 1 5.37
CHEMBL5201164 1 5.27
CHEMBL5180005 1 5.21
CHEMBL5199659 1 5.03
CHEMBL5181746 1 4.97
CHEMBL5174172 1 4.82
CHEMBL5186267 1 4.80
CHEMBL5205731 1 4.71
CHEMBL5209233 1 4.63
CHEMBL5175703 1 4.63
CHEMBL4465054 1 4.62
CHEMBL5174023 1 4.57
CHEMBL5182772 1 4.51
CHEMBL5180220 1 4.42
CHEMBL5175739 1 4.37
CHEMBL5191779 1 4.36
CHEMBL5183186 1 -
CHEMBL5191008 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188233 EC50 = 810.0 nM 6.09
CHEMBL5185127 EC50 = 1550.0 nM 5.81
CHEMBL5197904 EC50 = 3210.0 nM 5.49
CHEMBL5093161 EC50 = 4260.0 nM 5.37
CHEMBL5201164 EC50 = 5380.0 nM 5.27
CHEMBL5180005 EC50 = 6230.0 nM 5.21
CHEMBL5199659 EC50 = 9400.0 nM 5.03
CHEMBL5181746 EC50 = 10800.0 nM 4.97
CHEMBL5174172 EC50 = 15300.0 nM 4.82
CHEMBL5186267 EC50 = 15700.0 nM 4.80
CHEMBL5205731 EC50 = 19300.0 nM 4.71
CHEMBL5209233 EC50 = 23300.0 nM 4.63
CHEMBL5175703 EC50 = 23500.0 nM 4.63
CHEMBL4465054 EC50 = 24100.0 nM 4.62
CHEMBL5174023 EC50 = 26800.0 nM 4.57
CHEMBL5182772 EC50 = 31200.0 nM 4.51
CHEMBL5180220 EC50 = 38500.0 nM 4.42
CHEMBL5175739 EC50 = 42700.0 nM 4.37
CHEMBL5191779 EC50 = 43500.0 nM 4.36
CHEMBL5183186 EC50 > 100000.0 nM -
CHEMBL5191008 EC50 > 100000.0 nM -