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Assay Detail

CHEMBL5351772

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

Binding
Antagonist activity at rat alpha7 nACh receptor expressed in Xenopus oocyte assessed as inhibition of acetylcholine-induced response at -70 mV holding potential by voltage-clamp based electrophysiological assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
Xu P, Zhang P, Zhu X, Wu Y, Harvey PJ, Kaas Q, Zhangsun D, Craik DJ, Luo S.
J Med Chem (2023) 66 : 10092 -10107
PubMed 37464764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 5.56 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5427617 1 6.22
CHEMBL4460879 1 6.19
CHEMBL5436170 1 6.19
CHEMBL5396121 1 6.19
CHEMBL5407174 1 6.12
CHEMBL5439154 1 5.97
CHEMBL5426596 1 5.95
CHEMBL5409922 1 5.87
CHEMBL5403043 1 5.85
CHEMBL5419863 1 5.84
CHEMBL5428141 1 5.84
CHEMBL5426847 1 5.83
CHEMBL5398766 1 5.80
CHEMBL5404672 1 5.77
CHEMBL5432748 1 5.75
CHEMBL5435010 1 5.72
CHEMBL5406714 1 5.69
CHEMBL5426358 1 5.65
CHEMBL5401197 1 5.61
CHEMBL4553407 1 5.55
CHEMBL5394070 1 5.52
CHEMBL5440747 1 5.51
CHEMBL5396129 1 5.48
CHEMBL5413221 1 5.42
CHEMBL5422303 1 5.39
CHEMBL5396311 1 5.35
CHEMBL5428546 1 5.34
CHEMBL5435613 1 5.33
CHEMBL5432265 1 5.33
CHEMBL5423851 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5427617 IC50 = 600.0 nM 6.22
CHEMBL4460879 IC50 = 650.0 nM 6.19
CHEMBL5396121 IC50 = 640.0 nM 6.19
CHEMBL5436170 IC50 = 650.0 nM 6.19
CHEMBL5407174 IC50 = 760.0 nM 6.12
CHEMBL5439154 IC50 = 1080.0 nM 5.97
CHEMBL5426596 IC50 = 1130.0 nM 5.95
CHEMBL5409922 IC50 = 1360.0 nM 5.87
CHEMBL5403043 IC50 = 1420.0 nM 5.85
CHEMBL5419863 IC50 = 1450.0 nM 5.84
CHEMBL5428141 IC50 = 1460.0 nM 5.84
CHEMBL5426847 IC50 = 1470.0 nM 5.83
CHEMBL5398766 IC50 = 1600.0 nM 5.80
CHEMBL5404672 IC50 = 1700.0 nM 5.77
CHEMBL5432748 IC50 = 1780.0 nM 5.75
CHEMBL5435010 IC50 = 1910.0 nM 5.72
CHEMBL5406714 IC50 = 2060.0 nM 5.69
CHEMBL5426358 IC50 = 2250.0 nM 5.65
CHEMBL5401197 IC50 = 2450.0 nM 5.61
CHEMBL4553407 IC50 = 2830.0 nM 5.55
CHEMBL5394070 IC50 = 3030.0 nM 5.52
CHEMBL5440747 IC50 = 3080.0 nM 5.51
CHEMBL5396129 IC50 = 3280.0 nM 5.48
CHEMBL5413221 IC50 = 3780.0 nM 5.42
CHEMBL5422303 IC50 = 4100.0 nM 5.39
CHEMBL5396311 IC50 = 4480.0 nM 5.35
CHEMBL5428546 IC50 = 4520.0 nM 5.34
CHEMBL5435613 IC50 = 4680.0 nM 5.33
CHEMBL5432265 IC50 = 4620.0 nM 5.33
CHEMBL5423851 IC50 = 5610.0 nM 5.25
CHEMBL5413345 IC50 = 5600.0 nM 5.25
CHEMBL5419995 IC50 = 5720.0 nM 5.24
CHEMBL5416147 IC50 = 5890.0 nM 5.23
CHEMBL5393774 IC50 = 6330.0 nM 5.20
CHEMBL5400807 IC50 = 6440.0 nM 5.19
CHEMBL5394317 IC50 = 6690.0 nM 5.17
CHEMBL5427601 IC50 = 7130.0 nM 5.15
CHEMBL5431759 IC50 = 7330.0 nM 5.13
CHEMBL5394483 IC50 = 7640.0 nM 5.12
CHEMBL5420643 IC50 = 7640.0 nM 5.12
CHEMBL5417971 IC50 = 8760.0 nM 5.06
CHEMBL5425181 IC50 = 9050.0 nM 5.04
CHEMBL5414842 IC50 > 10000.0 nM -
CHEMBL5440425 IC50 > 10000.0 nM -
CHEMBL5423816 IC50 > 10000.0 nM -
CHEMBL5420679 IC50 > 10000.0 nM -
CHEMBL5422661 IC50 > 10000.0 nM -
CHEMBL5432876 IC50 > 10000.0 nM -