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

CHEMBL5041213

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

Binding
Inhibition of human Nav1.2 stably expressed in cells with train pulses to -20 mV at 0.1 Hz and holding potential of -95 mV by Qube-automated patch clamp assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 2 subunit alpha (CHEMBL4187)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na<sub>v</sub>1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM.
J Med Chem (2022) 65 : 485 -496
PubMed 34931831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.82 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318147 1 5.82
CHEMBL5085021 1 -
CHEMBL5076349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318147 IC50 = 1500.0 nM 5.82
CHEMBL5085021 IC50 > 17000.0 nM -
CHEMBL5076349 IC50 > 17000.0 nM -