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Assay Detail

CHEMBL5097928

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

Toxicity
Inhibition of hERG potassium channel assessed as maximum inhibition rate at -80 mV holding potential incubated for 120 seconds by whole cell-automated voltage clamp analysis assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-<i>b</i>]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens.
Kong Q, Pan W, Xu H, Xue Y, Guo B, Meng X, Luo C, Wang T, Zhang S, Yang Y.
J Med Chem (2021) 64 : 8644 -8665
PubMed 34080858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.34 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1200788 CISAPRIDE MONOHYDRATE 4.0 1 7.40
CHEMBL5208405 1 4.91
CHEMBL5189137 1 4.74
CHEMBL5179034 1 4.29
CHEMBL5173810 1 -
CHEMBL5198082 1 -
CHEMBL5195776 1 -
CHEMBL5175419 1 -
CHEMBL5187851 1 -
CHEMBL5180811 1 -
CHEMBL5173672 1 -
CHEMBL5172595 1 -
CHEMBL5180991 1 -
CHEMBL5209407 1 -
CHEMBL5190841 1 -
CHEMBL5183179 1 -
CHEMBL5186271 1 -
CHEMBL5181038 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1200788 CISAPRIDE MONOHYDRATE IC50 = 40.0 nM 7.40
CHEMBL5208405 IC50 = 12300.0 nM 4.91
CHEMBL5189137 IC50 = 18400.0 nM 4.74
CHEMBL5179034 IC50 = 51500.0 nM 4.29
CHEMBL5173810 IC50 > 40000.0 nM -
CHEMBL5198082 IC50 > 40000.0 nM -
CHEMBL5195776 IC50 > 40000.0 nM -
CHEMBL5175419 IC50 > 40000.0 nM -
CHEMBL5187851 IC50 > 40000.0 nM -
CHEMBL5180811 IC50 > 40000.0 nM -
CHEMBL5173672 IC50 > 40000.0 nM -
CHEMBL5172595 IC50 > 40000.0 nM -
CHEMBL5180991 IC50 > 40000.0 nM -
CHEMBL5209407 IC50 > 40000.0 nM -
CHEMBL5190841 IC50 > 40000.0 nM -
CHEMBL5183179 IC50 > 40000.0 nM -
CHEMBL5186271 IC50 > 40000.0 nM -
CHEMBL5181038 IC50 > 40000.0 nM -