Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1041434

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

Binding
Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes
ChEMBL ↗
79
Total Activities
44
Compounds Tested
2
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

Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
Wang Y, Jones PJ, Batts TW, Landry V, Patel MK, Brown ML.
Bioorg Med Chem (2009) 17 : 7064 -7072
PubMed 19346132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 4.84 5.85
pIC50 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1086 DIBUCAINE 4.0 2 5.85
CHEMBL1196 PROPARACAINE 4.0 2 5.72
CHEMBL698 TETRACAINE 4.0 2 5.47
CHEMBL492 ETIDOCAINE 4.0 2 5.46
CHEMBL417155 — — 2 5.30
CHEMBL610750 — — 2 5.30
CHEMBL1098 BUPIVACAINE 4.0 2 5.27
CHEMBL596058 — — 1 5.22
CHEMBL1197 HEXYLCAINE 4.0 2 5.15
CHEMBL287713 — — 2 5.05
CHEMBL289499 — — 2 4.89
CHEMBL127865 PIPEROCAINE 2.0 2 4.89
CHEMBL593347 — — 1 4.87
CHEMBL421669 PARETHOXYCAINE 2.0 2 4.62
CHEMBL1769 PROPOXYCAINE HYDROCHLORIDE 4.0 2 4.62
CHEMBL594410 — — 2 4.41
CHEMBL593479 — — 1 4.40
CHEMBL16 PHENYTOIN 4.0 2 4.40
CHEMBL595810 — — 1 4.40
CHEMBL370805 COCAINE 4.0 2 4.31
CHEMBL1093 ARTICAINE 4.0 2 4.29
CHEMBL1194 PRILOCAINE 4.0 2 4.27
CHEMBL39326 — — 2 4.24
CHEMBL39889 — — 2 4.24
CHEMBL39247 — — 2 4.02
CHEMBL605523 — — 1 -
CHEMBL593147 — — 1 -
CHEMBL603533 — — 1 -
CHEMBL607254 — — 1 -
CHEMBL596330 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1086 DIBUCAINE IC50 = 1412.54 nM 5.85
CHEMBL1086 DIBUCAINE IC50 = 1400.0 nM 5.85
CHEMBL1196 PROPARACAINE IC50 = 1905.46 nM 5.72
CHEMBL1196 PROPARACAINE IC50 = 2000.0 nM 5.70
CHEMBL698 TETRACAINE IC50 = 3400.0 nM 5.47
CHEMBL698 TETRACAINE IC50 = 3388.44 nM 5.47
CHEMBL492 ETIDOCAINE IC50 = 3500.0 nM 5.46
CHEMBL492 ETIDOCAINE IC50 = 3467.37 nM 5.46
CHEMBL417155 — IC50 = 5011.87 nM 5.30
CHEMBL610750 — IC50 = 5011.87 nM 5.30
CHEMBL610750 — IC50 = 5000.0 nM 5.30
CHEMBL417155 — IC50 = 5000.0 nM 5.30
CHEMBL1098 BUPIVACAINE IC50 = 5370.32 nM 5.27
CHEMBL1098 BUPIVACAINE IC50 = 5400.0 nM 5.27
CHEMBL596058 — IC50 = 6025.6 nM 5.22
CHEMBL1197 HEXYLCAINE IC50 = 7079.46 nM 5.15
CHEMBL1197 HEXYLCAINE IC50 = 7100.0 nM 5.15
CHEMBL287713 — IC50 = 8912.51 nM 5.05
CHEMBL287713 — IC50 = 9000.0 nM 5.05
CHEMBL127865 PIPEROCAINE IC50 = 12882.5 nM 4.89
CHEMBL127865 PIPEROCAINE IC50 = 12900.0 nM 4.89
CHEMBL289499 — IC50 = 12882.5 nM 4.89
CHEMBL289499 — IC50 = 13000.0 nM 4.89
CHEMBL593347 — IC50 = 13489.63 nM 4.87
CHEMBL1769 PROPOXYCAINE HYDROCHLORIDE IC50 = 24000.0 nM 4.62
CHEMBL421669 PARETHOXYCAINE IC50 = 24000.0 nM 4.62
CHEMBL421669 PARETHOXYCAINE IC50 = 23988.33 nM 4.62
CHEMBL1769 PROPOXYCAINE HYDROCHLORIDE IC50 = 23988.33 nM 4.62
CHEMBL594410 — IC50 = 38904.51 nM 4.41
CHEMBL594410 — IC50 = 39000.0 nM 4.41
CHEMBL595810 — IC50 = 39810.72 nM 4.40
CHEMBL593479 — IC50 = 39810.72 nM 4.40
CHEMBL16 PHENYTOIN IC50 = 40000.0 nM 4.40
CHEMBL16 PHENYTOIN IC50 = 39810.72 nM 4.40
CHEMBL370805 COCAINE IC50 = 48977.88 nM 4.31
CHEMBL370805 COCAINE IC50 = 49000.0 nM 4.31
CHEMBL1093 ARTICAINE IC50 = 51286.14 nM 4.29
CHEMBL1093 ARTICAINE IC50 = 51000.0 nM 4.29
CHEMBL1194 PRILOCAINE IC50 = 53700.0 nM 4.27
CHEMBL1194 PRILOCAINE IC50 = 53703.18 nM 4.27
CHEMBL39326 — IC50 = 57543.99 nM 4.24
CHEMBL39889 — IC50 = 57543.99 nM 4.24
CHEMBL39326 — IC50 = 58000.0 nM 4.24
CHEMBL39889 — IC50 = 58000.0 nM 4.24
CHEMBL39247 — IC50 = 95000.0 nM 4.02
CHEMBL39247 — IC50 = 95499.26 nM 4.02
CHEMBL290090 — IC50 = 251000.0 nM -
CHEMBL79 LIDOCAINE IC50 = 239883.29 nM -
CHEMBL39377 — IC50 = 251000.0 nM -
CHEMBL290743 — IC50 = 250000.0 nM -