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Assay Detail

CHEMBL4706334

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

Binding
Binding affinity to C-terminal His6 tagged CAL PDZ 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

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 7.39 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756359 1 8.22
CHEMBL4763464 1 7.31
CHEMBL4789294 1 7.06
CHEMBL4756115 1 6.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756359 Kd = 6.0 nM 8.22
CHEMBL4763464 Kd = 49.0 nM 7.31
CHEMBL4789294 Kd = 87.0 nM 7.06
CHEMBL4756115 Kd = 113.0 nM 6.95