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

CHEMBL1772131

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

Binding
Inhibition of human ASIC3 expressed in HEK293 cells assessed as inhibition of acid-evoked current by manual patch-clamp electrophysiology assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acid-sensing ion channel 3 (CHEMBL5368)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Wolkenberg SE, Zhao Z, Mulhearn JJ, Harrison ST, Sanders JM, Cato MJ, Jovanovska A, Panigel J, Cook SP, Henze DA, Kane SA, Hartman GD, Barrow JC.
Bioorg Med Chem Lett (2011) 21 : 2646 -2649
PubMed 21257308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.65 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1770740 1 5.92
CHEMBL1770745 1 5.77
CHEMBL1770739 1 5.58
CHEMBL1770750 1 5.51
CHEMBL1770744 1 5.48
CHEMBL1770752 1 5.42
CHEMBL1770741 1 5.24
CHEMBL1770738 1 5.16
CHEMBL1770746 1 5.15
CHEMBL1770730 1 5.05
CHEMBL1770753 1 5.02
CHEMBL1770743 1 4.96
CHEMBL1770749 1 4.84
CHEMBL1770751 1 4.77
CHEMBL1770748 1 4.71
CHEMBL1770742 1 4.56
CHEMBL1770735 1 4.01
CHEMBL1770733 1 3.89
CHEMBL1770737 1 3.80
CHEMBL196536 1 3.72
CHEMBL1770734 1 3.44
CHEMBL1770736 1 3.37
CHEMBL1770731 1 3.15
CHEMBL1671950 1 3.12
CHEMBL1770747 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1770740 IC50 = 1200.0 nM 5.92
CHEMBL1770745 IC50 = 1700.0 nM 5.77
CHEMBL1770739 IC50 = 2600.0 nM 5.58
CHEMBL1770750 IC50 = 3100.0 nM 5.51
CHEMBL1770744 IC50 = 3300.0 nM 5.48
CHEMBL1770752 IC50 = 3800.0 nM 5.42
CHEMBL1770741 IC50 = 5800.0 nM 5.24
CHEMBL1770738 IC50 = 6900.0 nM 5.16
CHEMBL1770746 IC50 = 7100.0 nM 5.15
CHEMBL1770730 IC50 = 9000.0 nM 5.05
CHEMBL1770753 IC50 = 9600.0 nM 5.02
CHEMBL1770743 IC50 = 10900.0 nM 4.96
CHEMBL1770749 IC50 = 14400.0 nM 4.84
CHEMBL1770751 IC50 = 17000.0 nM 4.77
CHEMBL1770748 IC50 = 19400.0 nM 4.71
CHEMBL1770742 IC50 = 27600.0 nM 4.56
CHEMBL1770735 IC50 = 97000.0 nM 4.01
CHEMBL1770733 IC50 = 130000.0 nM 3.89
CHEMBL1770737 IC50 = 160000.0 nM 3.80
CHEMBL196536 IC50 = 190000.0 nM 3.72
CHEMBL1770734 IC50 = 363000.0 nM 3.44
CHEMBL1770736 IC50 = 430000.0 nM 3.37
CHEMBL1770731 IC50 = 701000.0 nM 3.15
CHEMBL1671950 IC50 = 763000.0 nM 3.12
CHEMBL1770747 IC50 = 103000.0 nM -