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Assay Detail

CHEMBL5038533

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

Binding
Inhibition on hERG expressed in HEK293 cells by Qpatch method
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery and Evaluation of Novel Angular Fused Pyridoquinazolinonecarboxamides as RNA Polymerase I Inhibitors.
Dorado TE, de León P, Begum A, Liu H, Chen D, Rajeshkumar NV, Rey-Rodriguez R, Hoareau-Aveilla C, Alcouffe C, Laiho M, Barrow JC.
ACS Med Chem Lett (2022) 13 : 608 -614
PubMed 35450366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.32 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091818 1 5.44
CHEMBL5091051 1 5.43
CHEMBL5074659 1 5.42
CHEMBL5075517 1 5.40
CHEMBL5092554 1 5.35
CHEMBL5091256 1 5.34
CHEMBL5081532 1 5.25
CHEMBL5087053 1 5.13
CHEMBL5089676 1 5.08
CHEMBL5089702 1 -
CHEMBL5072152 1 -
CHEMBL5072616 1 -
CHEMBL5072213 1 -
CHEMBL5082744 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091818 IC50 = 3640.0 nM 5.44
CHEMBL5091051 IC50 = 3720.0 nM 5.43
CHEMBL5074659 IC50 = 3800.0 nM 5.42
CHEMBL5075517 IC50 = 3970.0 nM 5.40
CHEMBL5092554 IC50 = 4440.0 nM 5.35
CHEMBL5091256 IC50 = 4530.0 nM 5.34
CHEMBL5081532 IC50 = 5570.0 nM 5.25
CHEMBL5087053 IC50 = 7390.0 nM 5.13
CHEMBL5089676 IC50 = 8260.0 nM 5.08
CHEMBL5089702 IC50 > 10000.0 nM -
CHEMBL5072152 IC50 > 10000.0 nM -
CHEMBL5072616 IC50 > 10000.0 nM -
CHEMBL5072213 IC50 > 10000.0 nM -
CHEMBL5082744 IC50 > 10000.0 nM -