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Assay Detail

CHEMBL918668

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

Binding
Displacement of [3H]BTX-B from voltage gated sodium channel in rat cerebral cortex synaptoneurosomes
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationship studies for hydantoins and analogues as voltage-gated sodium channel ligands.
Zha C, Brown GB, Brouillette WJ.
J Med Chem (2004) 47 : 6519 -6528
PubMed 15588087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 5.14 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225189 1 6.66
CHEMBL225170 1 5.96
CHEMBL373877 1 5.89
CHEMBL225495 1 5.66
CHEMBL225408 1 5.60
CHEMBL376544 1 5.48
CHEMBL222105 1 5.37
CHEMBL222210 1 5.35
CHEMBL425125 1 5.32
CHEMBL39043 1 5.30
CHEMBL225405 1 5.30
CHEMBL417155 1 5.30
CHEMBL374113 1 5.29
CHEMBL540451 1 5.28
CHEMBL225197 1 5.20
CHEMBL222208 1 5.19
CHEMBL373380 1 5.16
CHEMBL387956 1 5.09
CHEMBL287713 1 5.05
CHEMBL388171 1 4.96
CHEMBL388327 1 4.96
CHEMBL376661 1 4.89
CHEMBL376872 1 4.52
CHEMBL376560 1 4.52
CHEMBL373470 1 4.46
CHEMBL225389 1 4.44
CHEMBL288505 1 4.41
CHEMBL224836 1 4.29
CHEMBL222910 1 4.08
CHEMBL288861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225189 IC50 = 220.0 nM 6.66
CHEMBL225170 IC50 = 1100.0 nM 5.96
CHEMBL373877 IC50 = 1300.0 nM 5.89
CHEMBL225495 IC50 = 2200.0 nM 5.66
CHEMBL225408 IC50 = 2500.0 nM 5.60
CHEMBL376544 IC50 = 3300.0 nM 5.48
CHEMBL222105 IC50 = 4300.0 nM 5.37
CHEMBL222210 IC50 = 4500.0 nM 5.35
CHEMBL425125 IC50 = 4800.0 nM 5.32
CHEMBL39043 IC50 = 5000.0 nM 5.30
CHEMBL225405 IC50 = 5000.0 nM 5.30
CHEMBL417155 IC50 = 5000.0 nM 5.30
CHEMBL374113 IC50 = 5100.0 nM 5.29
CHEMBL540451 IC50 = 5300.0 nM 5.28
CHEMBL225197 IC50 = 6300.0 nM 5.20
CHEMBL222208 IC50 = 6500.0 nM 5.19
CHEMBL373380 IC50 = 6900.0 nM 5.16
CHEMBL387956 IC50 = 8200.0 nM 5.09
CHEMBL287713 IC50 = 9000.0 nM 5.05
CHEMBL388171 IC50 = 11000.0 nM 4.96
CHEMBL388327 IC50 = 11000.0 nM 4.96
CHEMBL376661 IC50 = 13000.0 nM 4.89
CHEMBL376872 IC50 = 30000.0 nM 4.52
CHEMBL376560 IC50 = 30000.0 nM 4.52
CHEMBL373470 IC50 = 35000.0 nM 4.46
CHEMBL225389 IC50 = 36000.0 nM 4.44
CHEMBL288505 IC50 = 39000.0 nM 4.41
CHEMBL224836 IC50 = 51000.0 nM 4.29
CHEMBL222910 IC50 = 84000.0 nM 4.08
CHEMBL221785 IC50 = 178000.0 nM -
CHEMBL225140 IC50 > 500000.0 nM -
CHEMBL445584 IC50 = 500000.0 nM -
CHEMBL225253 IC50 > 500000.0 nM -
CHEMBL225648 IC50 > 500000.0 nM -
CHEMBL275861 IC50 > 500000.0 nM -
CHEMBL224848 IC50 > 500000.0 nM -
CHEMBL1438 IC50 > 200000.0 nM -
CHEMBL221365 IC50 > 500000.0 nM -
CHEMBL390536 IC50 = 500000.0 nM -
CHEMBL222042 IC50 = 274000.0 nM -
CHEMBL222770 IC50 = 112000.0 nM -
CHEMBL309487 ATROLACTAMIDE IC50 > 500000.0 nM -
CHEMBL221361 IC50 > 200000.0 nM -
CHEMBL222263 IC50 = 448000.0 nM -
CHEMBL374202 IC50 = 112000.0 nM -
CHEMBL221456 IC50 = 300000.0 nM -
CHEMBL39010 IC50 = 103000.0 nM -
CHEMBL225586 IC50 > 500000.0 nM -
CHEMBL225585 IC50 > 500000.0 nM -
CHEMBL288861 IC50 = 162000.0 nM -