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Assay Detail

CHEMBL4193570

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

Binding
Inhibition of human Kv1.4 expressed in CHO cells at -80 mV holding potential by whole cell automated patch clamp method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Potassium voltage-gated channel subfamily A member 4 (CHEMBL4205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels.
Zidar N, Žula A, Tomašič T, Rogers M, Kirby RW, Tytgat J, Peigneur S, Kikelj D, Ilaš J, Mašič LP.
Eur J Med Chem (2017) 139 : 232 -241
PubMed 28802123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.29 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444449 1 6.77
CHEMBL4207745 1 5.82
CHEMBL397591 OROIDIN 1 5.68
CHEMBL3621636 1 5.28
CHEMBL3261431 1 5.06
CHEMBL4213446 1 4.92
CHEMBL4208517 1 4.92
CHEMBL3261430 1 4.89
CHEMBL4202870 1 4.82
CHEMBL4210636 1 4.77
CHEMBL465679 CLATHRODIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444449 IC50 = 170.0 nM 6.77
CHEMBL4207745 IC50 = 1500.0 nM 5.82
CHEMBL397591 OROIDIN IC50 = 2100.0 nM 5.68
CHEMBL3621636 IC50 = 5300.0 nM 5.28
CHEMBL3261431 IC50 = 8800.0 nM 5.06
CHEMBL4213446 IC50 = 12000.0 nM 4.92
CHEMBL4208517 IC50 = 12000.0 nM 4.92
CHEMBL3261430 IC50 = 13000.0 nM 4.89
CHEMBL4202870 IC50 = 15000.0 nM 4.82
CHEMBL4210636 IC50 = 17000.0 nM 4.77
CHEMBL465679 CLATHRODIN IC50 > 30000.0 nM -