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Assay Detail

CHEMBL821185

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

Binding
Dissociation constant for the blockage of voltage-gated potassium channel subunit Kv1.3 in human lymphocytes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Potassium voltage-gated channel subfamily A member 3 (CHEMBL4633)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activity.
Baell JB, Gable RW, Harvey AJ, Toovey N, Herzog T, Hänsel W, Wulff H.
J Med Chem (2004) 47 : 2326 -2336
PubMed 15084131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 27 5.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311283 CORREOLIDE 1 7.00
CHEMBL308029 1 6.55
CHEMBL310916 1 6.40
CHEMBL306931 1 6.25
CHEMBL76997 1 6.22
CHEMBL307016 1 6.17
CHEMBL78325 1 6.16
CHEMBL432341 1 6.16
CHEMBL77926 1 6.10
CHEMBL76543 1 6.10
CHEMBL77317 1 6.09
CHEMBL72328 1 6.00
CHEMBL75091 1 6.00
CHEMBL308554 1 5.82
CHEMBL306037 1 5.70
CHEMBL78004 1 5.52
CHEMBL75159 1 5.51
CHEMBL78267 1 5.46
CHEMBL74306 1 5.40
CHEMBL77493 1 5.30
CHEMBL306038 1 5.15
CHEMBL77572 1 5.00
CHEMBL306708 1 4.77
CHEMBL78293 1 4.30
CHEMBL310762 1 4.16
CHEMBL422416 1 4.00
CHEMBL284348 DALFAMPRIDINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311283 CORREOLIDE Kd = 100.0 nM 7.00
CHEMBL308029 Kd = 280.0 nM 6.55
CHEMBL310916 Kd = 400.0 nM 6.40
CHEMBL306931 Kd = 560.0 nM 6.25
CHEMBL76997 Kd = 600.0 nM 6.22
CHEMBL307016 Kd = 680.0 nM 6.17
CHEMBL78325 Kd = 700.0 nM 6.16
CHEMBL432341 Kd = 700.0 nM 6.16
CHEMBL77926 Kd = 800.0 nM 6.10
CHEMBL76543 Kd = 800.0 nM 6.10
CHEMBL77317 Kd = 820.0 nM 6.09
CHEMBL72328 Kd = 1000.0 nM 6.00
CHEMBL75091 Kd = 1000.0 nM 6.00
CHEMBL308554 Kd = 1500.0 nM 5.82
CHEMBL306037 Kd = 2000.0 nM 5.70
CHEMBL78004 Kd = 3000.0 nM 5.52
CHEMBL75159 Kd = 3100.0 nM 5.51
CHEMBL78267 Kd = 3500.0 nM 5.46
CHEMBL74306 Kd = 4000.0 nM 5.40
CHEMBL77493 Kd = 5000.0 nM 5.30
CHEMBL306038 Kd = 7100.0 nM 5.15
CHEMBL77572 Kd = 10000.0 nM 5.00
CHEMBL306708 Kd = 17000.0 nM 4.77
CHEMBL78293 Kd = 50000.0 nM 4.30
CHEMBL310762 Kd = 70000.0 nM 4.16
CHEMBL422416 Kd = 100000.0 nM 4.00
CHEMBL284348 DALFAMPRIDINE Kd = 195000.0 nM -