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Assay Detail

CHEMBL2389045

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

Binding
Antagonist activity at Gloeobacter violaceus ligand-gated ion channel expressed in Xenopus oocytes assessed as inhibition of MES buffer pH 5.5 -induced currents after 30 secs by voltage clamp technique
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Gloeobacter violaceus
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of cinnamic acid derivatives as novel antagonists of the prokaryotic proton-gated ion channel GLIC.
Prevost MS, Delarue-Cochin S, Marteaux J, Colas C, Van Renterghem C, Blondel A, Malliavin T, Corringer PJ, Joseph D.
J Med Chem (2013) 56 : 4619 -4630
PubMed 23682762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.49 5.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66879 COUMARIC ACID 1 5.02
CHEMBL233295 ISOFERULIC ACID 1 4.87
CHEMBL1771752 3-CHLORO-CINNAMIC ACID 1 4.86
CHEMBL145 CAFFEIC ACID 3.0 1 4.78
CHEMBL2387748 1 4.60
CHEMBL1173153 1 4.54
CHEMBL27246 CINNAMIC ACID 1 4.46
CHEMBL173521 1 4.27
CHEMBL114648 BETA-NAPHTOIC ACID 1 4.21
CHEMBL1321891 1 4.13
CHEMBL2387750 1 4.08
CHEMBL136927 DIHYDROCAFFEIC ACID 1 4.06
CHEMBL17001 METHYLCAFFEATE 1 -
CHEMBL17347 ETHYL CAFFEATE 1 -
CHEMBL305202 1 -
CHEMBL2387747 CINNAMONITRILE 1 -
CHEMBL1778420 1 -
CHEMBL2148183 1 -
CHEMBL2387749 (E)-N-METHOXYCINNAMAMIDE 1 -
CHEMBL320295 O,O'-DIMETHYLCAFFEIC ACID 1 -
CHEMBL1234624 1 -
CHEMBL83294 COUMARIN-3-CARBOXYLIC ACID 1 -
CHEMBL1160352 1 -
CHEMBL1830821 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66879 COUMARIC ACID IC50 = 9590.0 nM 5.02
CHEMBL233295 ISOFERULIC ACID IC50 = 13500.0 nM 4.87
CHEMBL1771752 3-CHLORO-CINNAMIC ACID IC50 = 13700.0 nM 4.86
CHEMBL145 CAFFEIC ACID IC50 = 16700.0 nM 4.78
CHEMBL2387748 IC50 = 25300.0 nM 4.60
CHEMBL1173153 IC50 = 28800.0 nM 4.54
CHEMBL27246 CINNAMIC ACID IC50 = 34600.0 nM 4.46
CHEMBL173521 IC50 = 53300.0 nM 4.27
CHEMBL114648 BETA-NAPHTOIC ACID IC50 = 61400.0 nM 4.21
CHEMBL1321891 IC50 = 73900.0 nM 4.13
CHEMBL2387750 IC50 = 83500.0 nM 4.08
CHEMBL136927 DIHYDROCAFFEIC ACID IC50 = 86800.0 nM 4.06
CHEMBL17001 METHYLCAFFEATE IC50 = 388000.0 nM -
CHEMBL17347 ETHYL CAFFEATE IC50 = 246000.0 nM -
CHEMBL305202 IC50 = 295000.0 nM -
CHEMBL2387747 CINNAMONITRILE IC50 - -
CHEMBL1778420 IC50 - -
CHEMBL2148183 IC50 = 7940000.0 nM -
CHEMBL2387749 (E)-N-METHOXYCINNAMAMIDE IC50 - -
CHEMBL320295 O,O'-DIMETHYLCAFFEIC ACID IC50 = 206000.0 nM -
CHEMBL1234624 IC50 - -
CHEMBL83294 COUMARIN-3-CARBOXYLIC ACID IC50 = 282000.0 nM -
CHEMBL1160352 IC50 = 347000.0 nM -
CHEMBL1830821 IC50 = 168000.0 nM -