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Assay Detail

CHEMBL4817543

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Functional
Antiproliferative activity against human Caco-2 cells expressing wild type KRAS assessed as reduction in cell growth incubated for 72 hrs by CyQuant proliferation assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Caco-2
Confidence 1 — Organism
Curated By Autocuration

Target

Caco-2 (CHEMBL614058)
Type CELL-LINE
Organism Homo sapiens

Publication

Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.
Wang P, van der Hoeven D, Ye N, Chen H, Liu Z, Ma X, Montufar-Solis D, Rehl KM, Cho KJ, Thapa S, Chen W, van der Hoeven R, Frost JA, Hancock JF, Zhou J.
Eur J Med Chem (2021) 217 : 113381 -113381
PubMed 33756124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.22 5.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4859726 1 5.38
CHEMBL4854753 1 5.36
CHEMBL4858481 1 5.29
CHEMBL254832 FENDILINE 2.0 1 4.84
CHEMBL4849536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4859726 IC50 = 4200.0 nM 5.38
CHEMBL4854753 IC50 = 4400.0 nM 5.36
CHEMBL4858481 IC50 = 5100.0 nM 5.29
CHEMBL254832 FENDILINE IC50 = 14500.0 nM 4.84
CHEMBL4849536 IC50 > 30000.0 nM -