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Assay Detail

CHEMBL4220449

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Functional
Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COLO 205
Confidence 1 — Organism
Curated By Intermediate

Target

COLO 205 (CHEMBL614561)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold.
Lu B, Huang S, Cao J, Hu Q, Shen R, Wan H, Wang D, Yuan J, Zhang L, Zhang J, Zhang M, Tao W, Zhang L.
Bioorg Med Chem (2018) 26 : 581 -589
PubMed 29317148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.83 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228425 1 8.60
CHEMBL4229260 1 8.54
CHEMBL4228999 1 8.33
CHEMBL4225401 1 8.14
CHEMBL4225654 1 8.00
CHEMBL4228161 1 7.92
CHEMBL4225180 1 7.42
CHEMBL1614701 SELUMETINIB 4.0 1 7.23
CHEMBL4225400 1 7.12
CHEMBL4226300 1 7.04
CHEMBL4227816 1 -
CHEMBL4226967 1 -
CHEMBL4227199 1 -
CHEMBL4228687 1 -
CHEMBL4224923 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228425 IC50 = 2.5 nM 8.60
CHEMBL4229260 IC50 = 2.9 nM 8.54
CHEMBL4228999 IC50 = 4.7 nM 8.33
CHEMBL4225401 IC50 = 7.2 nM 8.14
CHEMBL4225654 IC50 = 10.0 nM 8.00
CHEMBL4228161 IC50 = 12.0 nM 7.92
CHEMBL4225180 IC50 = 38.4 nM 7.42
CHEMBL1614701 SELUMETINIB IC50 = 59.0 nM 7.23
CHEMBL4225400 IC50 = 76.5 nM 7.12
CHEMBL4226300 IC50 = 90.1 nM 7.04
CHEMBL4227816 IC50 > 1000.0 nM -
CHEMBL4226967 IC50 - -
CHEMBL4227199 IC50 - -
CHEMBL4228687 IC50 > 1000.0 nM -
CHEMBL4224923 IC50 > 1000.0 nM -