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Assay Detail

CHEMBL4412206

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Functional
Antiproliferative activity against human A549 cells harboring KRAS G12S point mutant after 72 hrs by SRB assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.
Chen D, Chen Y, Lian F, Chen L, Li Y, Cao D, Wang X, Chen L, Li J, Meng T, Huang M, Geng M, Shen J, Zhang N, Xiong B.
Eur J Med Chem (2019) 163 : 597 -609
PubMed 30562696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.76 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3286929 1 5.19
CHEMBL4450839 1 4.99
CHEMBL4527667 1 4.95
CHEMBL4439169 1 4.77
CHEMBL4443518 1 4.74
CHEMBL4459864 1 4.71
CHEMBL4566147 1 4.69
CHEMBL4449262 1 4.62
CHEMBL4536719 1 4.49
CHEMBL4514611 1 4.44
CHEMBL4555739 1 -
CHEMBL4532027 1 -
CHEMBL4589625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3286929 IC50 = 6400.0 nM 5.19
CHEMBL4450839 IC50 = 10300.0 nM 4.99
CHEMBL4527667 IC50 = 11300.0 nM 4.95
CHEMBL4439169 IC50 = 17100.0 nM 4.77
CHEMBL4443518 IC50 = 18300.0 nM 4.74
CHEMBL4459864 IC50 = 19300.0 nM 4.71
CHEMBL4566147 IC50 = 20300.0 nM 4.69
CHEMBL4449262 IC50 = 24100.0 nM 4.62
CHEMBL4536719 IC50 = 32600.0 nM 4.49
CHEMBL4514611 IC50 = 36000.0 nM 4.44
CHEMBL4555739 IC50 > 50000.0 nM -
CHEMBL4532027 IC50 > 50000.0 nM -
CHEMBL4589625 IC50 > 50000.0 nM -