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Assay Detail

CHEMBL4340216

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

Binding
Inhibition of pH 6.25-stimulated mouse ASIC1a/2a heterodimer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Acid-sensing ion channel 1/2 (CHEMBL4523651)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS.
Bencheva LI, De Matteo M, Ferrante L, Ferrara M, Prandi A, Randazzo P, Ronzoni S, Sinisi R, Seneci P, Summa V, Gallo M, Veneziano M, Cellucci A, Mazzocchi N, Menegon A, Di Fabio R.
ACS Med Chem Lett (2019) 10 : 627 -632
PubMed 30996808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.83 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4445209 1 5.07
CHEMBL4518161 1 4.96
CHEMBL4528810 1 4.95
CHEMBL35241 DIMINAZENE 2.0 1 4.34
CHEMBL4456021 1 -
CHEMBL4590631 1 -
CHEMBL4538655 1 -
CHEMBL4469611 1 -
CHEMBL4476781 1 -
CHEMBL4593063 1 -
CHEMBL4446500 1 -
CHEMBL4591499 1 -
CHEMBL4593172 1 -
CHEMBL4524195 1 -
CHEMBL4555958 1 -
CHEMBL4462808 1 -
CHEMBL4450681 1 -
CHEMBL4587871 1 -
CHEMBL4440380 1 -
CHEMBL4463485 1 -
CHEMBL4517411 1 -
CHEMBL4442568 1 -
CHEMBL4463769 1 -
CHEMBL4527919 1 -
CHEMBL4440787 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4445209 IC50 = 8500.0 nM 5.07
CHEMBL4518161 IC50 = 10900.0 nM 4.96
CHEMBL4528810 IC50 = 11300.0 nM 4.95
CHEMBL35241 DIMINAZENE IC50 = 45200.0 nM 4.34
CHEMBL4456021 IC50 > 30000.0 nM -
CHEMBL4590631 IC50 > 30000.0 nM -
CHEMBL4538655 IC50 > 30000.0 nM -
CHEMBL4469611 IC50 > 30000.0 nM -
CHEMBL4476781 IC50 > 30000.0 nM -
CHEMBL4593063 IC50 > 30000.0 nM -
CHEMBL4446500 IC50 > 30000.0 nM -
CHEMBL4591499 IC50 > 30000.0 nM -
CHEMBL4593172 IC50 > 30000.0 nM -
CHEMBL4524195 IC50 > 30000.0 nM -
CHEMBL4555958 IC50 > 30000.0 nM -
CHEMBL4462808 IC50 > 30000.0 nM -
CHEMBL4450681 IC50 > 30000.0 nM -
CHEMBL4587871 IC50 > 30000.0 nM -
CHEMBL4440380 IC50 > 30000.0 nM -
CHEMBL4463485 IC50 > 30000.0 nM -
CHEMBL4517411 IC50 > 30000.0 nM -
CHEMBL4442568 IC50 > 30000.0 nM -
CHEMBL4463769 IC50 > 30000.0 nM -
CHEMBL4527919 IC50 > 30000.0 nM -
CHEMBL4440787 IC50 > 30000.0 nM -