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Assay Detail

CHEMBL5735811

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Binding
Electrophysiology Assay: Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons were isolated from the dorsal root ganglions and maintained in culture for 2 to 10 days in the presence of NGF (50 ng/ml) (culture media consisted of NeurobasalA supplemented with B27, glutamine and antibiotics). Small diameter neurons (nociceptors, 8-12 μm in diameter) were visually identified and probed with fine tip glass electrodes connected to an amplifier (Axon Instruments). The “voltage clamp” mode was used to assess the compound's IC50 holding the cells at −60 mV. In addition, the “current clamp” mode was employed to test the efficacy of the compounds in blocking action potential generation in response to current injections.
ChEMBL ↗
69
Total Activities
23
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Prodrugs of pyridone amides useful as modulators of sodium channels
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.59 9.00
kon 23 - -
k_off 23 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3678273 — — 3 9.00
CHEMBL3678270 — — 3 8.52
CHEMBL3915418 — — 3 8.40
CHEMBL3678272 — — 3 8.22
CHEMBL3678193 — — 3 7.96
CHEMBL3678240 — — 3 7.96
CHEMBL3678232 — — 3 7.89
CHEMBL3678234 — — 3 7.89
CHEMBL3678173 — — 3 7.85
CHEMBL3678194 — — 3 7.77
CHEMBL3678192 — — 3 7.55
CHEMBL6041444 — — 3 7.55
CHEMBL3678230 — — 3 7.52
CHEMBL3678183 — — 3 7.52
CHEMBL3678228 — — 3 7.43
CHEMBL5806212 — — 3 7.36
CHEMBL3678170 — — 3 7.30
CHEMBL3678236 — — 3 7.29
CHEMBL3678165 — — 3 7.27
CHEMBL3968604 — — 3 7.07
CHEMBL3901010 — — 3 6.48
CHEMBL3906455 — — 3 6.48
CHEMBL3961030 — — 3 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3678273 — IC50 = 1.0 nM 9.00
CHEMBL3678270 — IC50 = 3.0 nM 8.52
CHEMBL3915418 — IC50 = 4.0 nM 8.40
CHEMBL3678272 — IC50 = 6.0 nM 8.22
CHEMBL3678240 — IC50 = 11.0 nM 7.96
CHEMBL3678193 — IC50 = 11.0 nM 7.96
CHEMBL3678234 — IC50 = 13.0 nM 7.89
CHEMBL3678232 — IC50 = 13.0 nM 7.89
CHEMBL3678173 — IC50 = 14.0 nM 7.85
CHEMBL3678194 — IC50 = 17.0 nM 7.77
CHEMBL3678192 — IC50 = 28.0 nM 7.55
CHEMBL6041444 — IC50 = 28.0 nM 7.55
CHEMBL3678230 — IC50 = 30.0 nM 7.52
CHEMBL3678183 — IC50 = 30.0 nM 7.52
CHEMBL3678228 — IC50 = 37.0 nM 7.43
CHEMBL5806212 — IC50 = 44.0 nM 7.36
CHEMBL3678170 — IC50 = 50.0 nM 7.30
CHEMBL3678236 — IC50 = 51.0 nM 7.29
CHEMBL3678165 — IC50 = 54.0 nM 7.27
CHEMBL3968604 — IC50 = 86.0 nM 7.07
CHEMBL3901010 — IC50 = 329.0 nM 6.48
CHEMBL3906455 — IC50 = 330.0 nM 6.48
CHEMBL3961030 — IC50 = 457.0 nM 6.34
CHEMBL3678236 — k_off = - s-1 -
CHEMBL5806212 — kon = - — -
CHEMBL5806212 — k_off = - s-1 -
CHEMBL3678236 — kon = - — -
CHEMBL3678170 — kon = - — -
CHEMBL3678240 — k_off = - s-1 -
CHEMBL3915418 — kon = - — -
CHEMBL3915418 — k_off = - s-1 -
CHEMBL3678273 — kon = - — -
CHEMBL3678273 — k_off = - s-1 -
CHEMBL6041444 — kon = - — -
CHEMBL6041444 — k_off = - s-1 -
CHEMBL3678270 — kon = - — -
CHEMBL3678228 — k_off = - s-1 -
CHEMBL3678228 — kon = - — -
CHEMBL3678183 — k_off = - s-1 -
CHEMBL3678183 — kon = - — -
CHEMBL3961030 — kon = - — -
CHEMBL3961030 — k_off = - s-1 -
CHEMBL3901010 — k_off = - s-1 -
CHEMBL3968604 — kon = - — -
CHEMBL3901010 — kon = - — -
CHEMBL3678165 — kon = - — -
CHEMBL3678170 — k_off = - s-1 -
CHEMBL3678230 — k_off = - s-1 -
CHEMBL3678165 — k_off = - s-1 -
CHEMBL3678230 — kon = - — -