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Assay Detail

CHEMBL4831907

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

Binding
Inhibition of mouse Panx-1 expressed in Xenopus laevis oocytes assessed as inhibition of membrane current cells held at -60 mV and voltage steps to +60 mV in presence of CBX measured by Whole cell voltage clamp assay relative to control
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Pannexin-1 (CHEMBL4879520)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of the first indole-based blockers of Panx-1 channel.
Crocetti L, Guerrini G, Puglioli S, Giovannoni MP, Di Cesare Mannelli L, Lucarini E, Ghelardini C, Wang J, Dahl G.
Eur J Med Chem (2021) 223 : 113650 -113650
PubMed 34174741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.33 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4855581 1 6.60
CHEMBL3184128 1 6.57
CHEMBL4847247 1 6.10
CHEMBL4858078 1 5.31
CHEMBL499915 CARBENOXOLONE 2.0 1 5.00
CHEMBL4862099 1 4.91
CHEMBL4849404 1 4.64
CHEMBL4873114 1 4.56
CHEMBL1256759 5-NITRO-2-PHENYLPROPYLAMINOBENZOIC ACID [NPPB] 1 4.30
CHEMBL897 PROBENECID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4855581 IC50 = 250.0 nM 6.60
CHEMBL3184128 IC50 = 270.0 nM 6.57
CHEMBL4847247 IC50 = 800.0 nM 6.10
CHEMBL4858078 IC50 = 4900.0 nM 5.31
CHEMBL499915 CARBENOXOLONE IC50 = 10000.0 nM 5.00
CHEMBL4862099 IC50 = 12400.0 nM 4.91
CHEMBL4849404 IC50 = 23100.0 nM 4.64
CHEMBL4873114 IC50 = 27500.0 nM 4.56
CHEMBL1256759 5-NITRO-2-PHENYLPROPYLAMINOBENZOIC ACID [NPPB] IC50 = 50000.0 nM 4.30
CHEMBL897 PROBENECID IC50 = 150000.0 nM -