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Assay Detail

CHEMBL4340096

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

Binding
Inhibition of NHERF1 in human SW620 cells expressing NHERF1 assessed as inhibition cell growth incubated for 72 hrs by MTT assay
7
Total Activities
7
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-RF1 (CHEMBL4523125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents.
Coluccia A, La Regina G, Naccarato V, Nalli M, Orlando V, Biagioni S, De Angelis ML, Baiocchi M, Gautier C, Gianni S, Di Pastena F, Di Magno L, Canettieri G, Coluccia AML, Silvestri R.
ACS Med Chem Lett (2019) 10 : 499 -503
PubMed 30996786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.66 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4539177 1 4.89
CHEMBL4456805 1 4.77
CHEMBL2363137 1 4.72
CHEMBL4536754 1 4.66
CHEMBL4584542 1 4.57
CHEMBL4449346 1 4.52
CHEMBL4527356 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4539177 IC50 = 13000.0 nM 4.89
CHEMBL4456805 IC50 = 17000.0 nM 4.77
CHEMBL2363137 IC50 = 19000.0 nM 4.72
CHEMBL4536754 IC50 = 22000.0 nM 4.66
CHEMBL4584542 IC50 = 27000.0 nM 4.57
CHEMBL4449346 IC50 = 30000.0 nM 4.52
CHEMBL4527356 IC50 = 31000.0 nM 4.51