Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4715076

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

Functional
Synergistic antiproliferative activity against human A549 cells harboring KRAS mutant assessed as reduction in cell viability in presence of 100 nM cobi-metinib
8
Total Activities
8
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

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Huestis MP,Durk MR,Eigenbrot C,Gibbons P,Hunsaker TL,La H,Leung DH,Liu W,Malek S,Merchant M,Moffat JG,Muli CS,Orr CJ,Parr BT,Shanahan F,Sneeringer CJ,Wang W,Yen I,Yin J,Rudolph J,Siu M
ACS Med Chem Lett (2021) 12 : 791 -797
PubMed 34055227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.64 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4740241 1 7.41
CHEMBL3577124 LY-3009120 1.0 1 7.34
CHEMBL4758903 1 6.86
CHEMBL4775998 1 6.83
CHEMBL4778772 1 6.73
CHEMBL4778419 1 6.43
CHEMBL4776565 1 5.95
CHEMBL4780060 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4740241 IC50 = 39.2 nM 7.41
CHEMBL3577124 LY-3009120 IC50 = 45.6 nM 7.34
CHEMBL4758903 IC50 = 138.0 nM 6.86
CHEMBL4775998 IC50 = 148.0 nM 6.83
CHEMBL4778772 IC50 = 187.0 nM 6.73
CHEMBL4778419 IC50 = 369.0 nM 6.43
CHEMBL4776565 IC50 = 1120.0 nM 5.95
CHEMBL4780060 IC50 = 2900.0 nM 5.54