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Assay Detail

CHEMBL4706336

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

Binding
Binding affinity to NHERF2 PDZ1 domain (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by fluorescence polarization based competition assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Na(+)/H(+) exchange regulatory cofactor NHE-RF2 (CHEMBL4739686)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic Peptidyl Inhibitors against CAL/CFTR Interaction for Treatment of Cystic Fibrosis.
Dougherty PG,Wellmerling JH,Koley A,Lukowski JK,Hummon AB,Cormet-Boyaka E,Pei D
J Med Chem (2020) 63 : 15773 -15784
PubMed 33314931 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.77 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4763464 1 6.25
CHEMBL4756359 1 5.86
CHEMBL4756115 1 5.73
CHEMBL4789294 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4763464 Kd = 560.0 nM 6.25
CHEMBL4756359 Kd = 1370.0 nM 5.86
CHEMBL4756115 Kd = 1870.0 nM 5.73
CHEMBL4789294 Kd = 6040.0 nM 5.22