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Assay Detail

CHEMBL4252297

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

Binding
Inhibition of DENV3 NS5 RdRp using ss-RNA PolyC as template and GTP as substrate assessed as decrease in dsRNA levels after 1 hr by PicoGreen-based fluorescence assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism dengue virus type 3
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Nonstructural protein 5 (CHEMBL4295629)
Type SINGLE PROTEIN
Organism Dengue virus

Publication

Functionalized 2,1-benzothiazine 2,2-dioxides as new inhibitors of Dengue NS5 RNA-dependent RNA polymerase.
Cannalire R, Tarantino D, Astolfi A, Barreca ML, Sabatini S, Massari S, Tabarrini O, Milani M, Querat G, Mastrangelo E, Manfroni G, Cecchetti V.
Eur J Med Chem (2018) 143 : 1667 -1676
PubMed 29137867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.12 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4288319 1 6.22
CHEMBL4292407 1 6.05
CHEMBL4281417 1 5.77
CHEMBL4279581 1 5.58
CHEMBL4289289 1 5.35
CHEMBL4284511 1 5.33
CHEMBL4281097 1 5.33
CHEMBL4284513 1 5.20
CHEMBL4280007 1 5.16
CHEMBL4281094 1 5.16
CHEMBL4295172 1 5.16
CHEMBL4289005 1 5.08
CHEMBL4291308 1 4.94
CHEMBL3233235 1 4.87
CHEMBL3233241 1 4.85
CHEMBL4277678 1 4.80
CHEMBL2326938 1 4.76
CHEMBL4291731 1 4.69
CHEMBL4287909 1 4.51
CHEMBL4277265 1 4.38
CHEMBL4280662 1 4.33
CHEMBL4287912 1 -
CHEMBL4287491 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4288319 IC50 = 600.0 nM 6.22
CHEMBL4292407 IC50 = 900.0 nM 6.05
CHEMBL4281417 IC50 = 1700.0 nM 5.77
CHEMBL4279581 IC50 = 2600.0 nM 5.58
CHEMBL4289289 IC50 = 4500.0 nM 5.35
CHEMBL4284511 IC50 = 4700.0 nM 5.33
CHEMBL4281097 IC50 = 4700.0 nM 5.33
CHEMBL4284513 IC50 = 6300.0 nM 5.20
CHEMBL4280007 IC50 = 7000.0 nM 5.16
CHEMBL4281094 IC50 = 6900.0 nM 5.16
CHEMBL4295172 IC50 = 7000.0 nM 5.16
CHEMBL4289005 IC50 = 8400.0 nM 5.08
CHEMBL4291308 IC50 = 11400.0 nM 4.94
CHEMBL3233235 IC50 = 13600.0 nM 4.87
CHEMBL3233241 IC50 = 14100.0 nM 4.85
CHEMBL4277678 IC50 = 15800.0 nM 4.80
CHEMBL2326938 IC50 = 17300.0 nM 4.76
CHEMBL4291731 IC50 = 20300.0 nM 4.69
CHEMBL4287909 IC50 = 30800.0 nM 4.51
CHEMBL4277265 IC50 = 41500.0 nM 4.38
CHEMBL4280662 IC50 = 46200.0 nM 4.33
CHEMBL4287912 IC50 > 50000.0 nM -
CHEMBL4287491 IC50 > 50000.0 nM -