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Assay Detail

CHEMBL1070909

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

Binding
Activation of KCNQ2/KCNQ3 expressed in CHO cells by isotopic efflux assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Publication

Novel KCNQ2/Q3 agonists as potential therapeutics for epilepsy and neuropathic pain.
Fritch PC, McNaughton-Smith G, Amato GS, Burns JF, Eargle CW, Roeloffs R, Harrison W, Jones L, Wickenden AD.
J Med Chem (2010) 53 : 887 -896
PubMed 20020710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 6.83 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL598553 1 7.68
CHEMBL592297 1 7.64
CHEMBL599164 1 7.60
CHEMBL598126 1 7.57
CHEMBL604937 1 7.55
CHEMBL599374 1 7.55
CHEMBL589898 1 7.54
CHEMBL591302 1 7.36
CHEMBL609624 1 7.36
CHEMBL599376 1 7.31
CHEMBL599781 1 7.28
CHEMBL599375 1 7.21
CHEMBL596909 1 7.04
CHEMBL602305 1 7.02
CHEMBL591203 1 7.01
CHEMBL589667 1 7.00
CHEMBL599365 1 6.80
CHEMBL603662 1 6.80
CHEMBL597341 1 6.66
CHEMBL592146 1 6.58
CHEMBL603661 1 6.42
CHEMBL602304 1 6.30
CHEMBL597329 1 6.24
CHEMBL608156 1 6.15
CHEMBL603667 1 5.68
CHEMBL603874 1 5.57
CHEMBL597342 1 5.25
CHEMBL597544 1 5.17
CHEMBL591677 1 -
CHEMBL597330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL598553 EC50 = 21.0 nM 7.68
CHEMBL592297 EC50 = 23.0 nM 7.64
CHEMBL599164 EC50 = 25.0 nM 7.60
CHEMBL598126 EC50 = 27.0 nM 7.57
CHEMBL604937 EC50 = 28.0 nM 7.55
CHEMBL599374 EC50 = 28.0 nM 7.55
CHEMBL589898 EC50 = 29.0 nM 7.54
CHEMBL591302 EC50 = 44.0 nM 7.36
CHEMBL609624 EC50 = 44.0 nM 7.36
CHEMBL599376 EC50 = 49.0 nM 7.31
CHEMBL599781 EC50 = 53.0 nM 7.28
CHEMBL599375 EC50 = 62.0 nM 7.21
CHEMBL596909 EC50 = 91.0 nM 7.04
CHEMBL602305 EC50 = 95.0 nM 7.02
CHEMBL591203 EC50 = 98.0 nM 7.01
CHEMBL589667 EC50 = 100.0 nM 7.00
CHEMBL599365 EC50 = 160.0 nM 6.80
CHEMBL603662 EC50 = 160.0 nM 6.80
CHEMBL597341 EC50 = 220.0 nM 6.66
CHEMBL592146 EC50 = 260.0 nM 6.58
CHEMBL603661 EC50 = 380.0 nM 6.42
CHEMBL602304 EC50 = 500.0 nM 6.30
CHEMBL597329 EC50 = 570.0 nM 6.24
CHEMBL608156 EC50 = 710.0 nM 6.15
CHEMBL603667 EC50 = 2080.0 nM 5.68
CHEMBL603874 EC50 = 2700.0 nM 5.57
CHEMBL597342 EC50 = 5570.0 nM 5.25
CHEMBL597544 EC50 = 6730.0 nM 5.17
CHEMBL591677 EC50 > 10000.0 nM -
CHEMBL597330 EC50 > 10000.0 nM -