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Assay Detail

CHEMBL861270

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Functional
Effect on blockade of mouse Kv1.3 channel expressed in L929 cells
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type L929
Confidence 9 — Direct single protein target
Curated By Expert

Target

Potassium voltage-gated channel subfamily A member 3 (CHEMBL4818) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.
Harvey AJ, Baell JB, Toovey N, Homerick D, Wulff H.
J Med Chem (2006) 49 : 1433 -1441
PubMed 16480279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 57 5.81 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426482 — — 1 6.40
CHEMBL373068 — — 1 6.38
CHEMBL202475 — — 1 6.38
CHEMBL202572 — — 1 6.35
CHEMBL382154 — — 1 6.32
CHEMBL202906 — — 1 6.30
CHEMBL205020 — — 1 6.30
CHEMBL201808 — — 1 6.30
CHEMBL381841 — — 1 6.29
CHEMBL440219 — — 1 6.26
CHEMBL203852 — — 1 6.22
CHEMBL203541 — — 1 6.22
CHEMBL203647 — — 1 6.22
CHEMBL204111 — — 1 6.17
CHEMBL202344 — — 1 6.16
CHEMBL204695 — — 1 6.16
CHEMBL426668 — — 1 6.16
CHEMBL204088 — — 1 6.12
CHEMBL201671 — — 1 6.10
CHEMBL204492 — — 1 6.05
CHEMBL438254 — — 1 6.00
CHEMBL202574 — — 1 6.00
CHEMBL426839 — — 1 6.00
CHEMBL380826 — — 1 5.96
CHEMBL381920 — — 1 5.92
CHEMBL203909 — — 1 5.92
CHEMBL201915 — — 1 5.92
CHEMBL424852 — — 1 5.92
CHEMBL379468 — — 1 5.92
CHEMBL383465 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426482 — EC50 = 400.0 nM 6.40
CHEMBL373068 — EC50 = 420.0 nM 6.38
CHEMBL202475 — EC50 = 420.0 nM 6.38
CHEMBL202572 — EC50 = 450.0 nM 6.35
CHEMBL382154 — EC50 = 480.0 nM 6.32
CHEMBL202906 — EC50 = 500.0 nM 6.30
CHEMBL205020 — EC50 = 500.0 nM 6.30
CHEMBL201808 — EC50 = 500.0 nM 6.30
CHEMBL381841 — EC50 = 510.0 nM 6.29
CHEMBL440219 — EC50 = 550.0 nM 6.26
CHEMBL203852 — EC50 = 600.0 nM 6.22
CHEMBL203541 — EC50 = 600.0 nM 6.22
CHEMBL203647 — EC50 = 600.0 nM 6.22
CHEMBL204111 — EC50 = 680.0 nM 6.17
CHEMBL426668 — EC50 = 700.0 nM 6.16
CHEMBL202344 — EC50 = 700.0 nM 6.16
CHEMBL204695 — EC50 = 700.0 nM 6.16
CHEMBL204088 — EC50 = 750.0 nM 6.12
CHEMBL201671 — EC50 = 800.0 nM 6.10
CHEMBL204492 — EC50 = 900.0 nM 6.05
CHEMBL438254 — EC50 = 1000.0 nM 6.00
CHEMBL202574 — EC50 = 1000.0 nM 6.00
CHEMBL426839 — EC50 = 1000.0 nM 6.00
CHEMBL380826 — EC50 = 1100.0 nM 5.96
CHEMBL383465 — EC50 = 1200.0 nM 5.92
CHEMBL203909 — EC50 = 1200.0 nM 5.92
CHEMBL379468 — EC50 = 1200.0 nM 5.92
CHEMBL201915 — EC50 = 1200.0 nM 5.92
CHEMBL381920 — EC50 = 1200.0 nM 5.92
CHEMBL424852 — EC50 = 1200.0 nM 5.92
CHEMBL202113 — EC50 = 1400.0 nM 5.85
CHEMBL202532 — EC50 = 1400.0 nM 5.85
CHEMBL381476 — EC50 = 1500.0 nM 5.82
CHEMBL425400 — EC50 = 1500.0 nM 5.82
CHEMBL204256 — EC50 = 1700.0 nM 5.77
CHEMBL382455 — EC50 = 1800.0 nM 5.75
CHEMBL204485 — EC50 = 1900.0 nM 5.72
CHEMBL204803 — EC50 = 2000.0 nM 5.70
CHEMBL380723 — EC50 = 2000.0 nM 5.70
CHEMBL203798 — EC50 = 2500.0 nM 5.60
CHEMBL381150 — EC50 = 2500.0 nM 5.60
CHEMBL204437 — EC50 = 2500.0 nM 5.60
CHEMBL382901 — EC50 = 3000.0 nM 5.52
CHEMBL203927 — EC50 = 4000.0 nM 5.40
CHEMBL204255 — EC50 = 5000.0 nM 5.30
CHEMBL382657 — EC50 = 5000.0 nM 5.30
CHEMBL425404 — EC50 = 5000.0 nM 5.30
CHEMBL201466 — EC50 = 5800.0 nM 5.24
CHEMBL205069 — EC50 = 6000.0 nM 5.22
CHEMBL204545 — EC50 = 6300.0 nM 5.20