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Assay Detail

CHEMBL5162430

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

Binding
Displacement of radiolabeled [3H]-2',3'-cGAMP from human STING HAQ variant incubated for 2 hrs by scintillation counting method
21
Total Activities
21
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

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
IC50 21 8.76 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5197904 1 9.00
CHEMBL5182772 1 8.96
CHEMBL5175703 1 8.92
CHEMBL5186267 1 8.89
CHEMBL5191779 1 8.89
CHEMBL5209233 1 8.89
CHEMBL4465054 1 8.74
CHEMBL5191008 1 8.62
CHEMBL5205731 1 8.47
CHEMBL5093161 1 8.22
CHEMBL5174172 1 -
CHEMBL5201164 1 -
CHEMBL5185127 1 -
CHEMBL5180220 1 -
CHEMBL5188233 1 -
CHEMBL5180005 1 -
CHEMBL5174023 1 -
CHEMBL5199659 1 -
CHEMBL5183186 1 -
CHEMBL5175739 1 -
CHEMBL5181746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5197904 IC50 = 1.0 nM 9.00
CHEMBL5182772 IC50 = 1.1 nM 8.96
CHEMBL5175703 IC50 = 1.2 nM 8.92
CHEMBL5186267 IC50 = 1.3 nM 8.89
CHEMBL5191779 IC50 = 1.3 nM 8.89
CHEMBL5209233 IC50 = 1.3 nM 8.89
CHEMBL4465054 IC50 = 1.8 nM 8.74
CHEMBL5191008 IC50 = 2.4 nM 8.62
CHEMBL5205731 IC50 = 3.4 nM 8.47
CHEMBL5093161 IC50 = 6.0 nM 8.22
CHEMBL5174172 IC50 < 1.0 nM -
CHEMBL5201164 IC50 < 1.0 nM -
CHEMBL5185127 IC50 < 1.0 nM -
CHEMBL5180220 IC50 < 1.0 nM -
CHEMBL5188233 IC50 < 1.0 nM -
CHEMBL5180005 IC50 < 1.0 nM -
CHEMBL5174023 IC50 < 1.0 nM -
CHEMBL5199659 IC50 < 1.0 nM -
CHEMBL5183186 IC50 < 1.0 nM -
CHEMBL5175739 IC50 < 1.0 nM -
CHEMBL5181746 IC50 < 1.0 nM -