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Assay Detail

CHEMBL833121

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

Functional
Effective concentration against whole-cell patch clamp from mouse HEK293 cells
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 1 — Organism
Curated By Intermediate

Target

HEK293 (CHEMBL614818)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides.
Wu YJ, Sun LQ, He H, Chen J, Starrett JE, Dextraze P, Daris JP, Boissard CG, Pieschl RL, Gribkoff VK, Natale J, Knox RJ, Harden DG, Thompson MW, Fitzpatrick W, Weaver D, Wu D, Gao Q, Dworetzky SI.
Bioorg Med Chem Lett (2004) 14 : 4533 -4537
PubMed 15357987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.62 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180886 2 7.70
CHEMBL176931 1 7.22
CHEMBL183979 1 6.48
CHEMBL363544 1 6.37
CHEMBL41355 EZOGABINE 4.0 1 5.89
CHEMBL317935 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180886 EC50 = 20.0 nM 7.70
CHEMBL176931 EC50 = 60.0 nM 7.22
CHEMBL180886 EC50 = 70.0 nM 7.16
CHEMBL183979 EC50 = 330.0 nM 6.48
CHEMBL363544 EC50 = 430.0 nM 6.37
CHEMBL41355 EZOGABINE EC50 = 1300.0 nM 5.89
CHEMBL317935 EC50 = 3200.0 nM 5.50