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

CHEMBL5588079

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

Functional
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant incubated for 72 hrs by CCK8 assay
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1<i>H</i>-benzo[<i>d</i>]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the "Clamp" Strategy.
Wang P, Yuan Y, Yang T, Zou Y, Tang M, Ma Z, Bo W, Qin S, Chen Y, Guo T, Guo Z, Yang J, Xiang M, Chen L.
J Med Chem (2024) 67 : 15246 -15267
PubMed 39166848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.55 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5596553 1 7.13
CHEMBL5597316 1 7.10
CHEMBL5597470 1 6.95
CHEMBL5596257 1 6.91
CHEMBL5598180 1 6.88
CHEMBL5596481 1 6.85
CHEMBL5596979 1 6.82
CHEMBL5596447 1 6.76
CHEMBL5597799 1 6.74
CHEMBL5596544 1 6.70
CHEMBL5597586 1 6.65
CHEMBL5596121 1 6.45
CHEMBL5598512 1 6.42
CHEMBL5597923 1 6.37
CHEMBL5597539 1 6.34
CHEMBL5597513 1 6.20
CHEMBL5598207 1 6.16
CHEMBL5598292 1 6.14
CHEMBL3264002 AVUTOMETINIB 3.0 1 6.13
CHEMBL5598214 1 6.05
CHEMBL3187723 BINIMETINIB 4.0 1 5.70
CHEMBL5597535 1 -
CHEMBL5598115 1 -
CHEMBL5596397 1 -
CHEMBL5596352 1 -
CHEMBL5597532 1 -
CHEMBL5591121 1 -
CHEMBL5597425 1 -
CHEMBL5597695 1 -
CHEMBL5598254 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5596553 IC50 = 74.0 nM 7.13
CHEMBL5597316 IC50 = 79.0 nM 7.10
CHEMBL5597470 IC50 = 113.0 nM 6.95
CHEMBL5596257 IC50 = 123.0 nM 6.91
CHEMBL5598180 IC50 = 132.0 nM 6.88
CHEMBL5596481 IC50 = 140.0 nM 6.85
CHEMBL5596979 IC50 = 150.0 nM 6.82
CHEMBL5596447 IC50 = 173.0 nM 6.76
CHEMBL5597799 IC50 = 183.0 nM 6.74
CHEMBL5596544 IC50 = 202.0 nM 6.70
CHEMBL5597586 IC50 = 223.0 nM 6.65
CHEMBL5596121 IC50 = 352.0 nM 6.45
CHEMBL5598512 IC50 = 377.0 nM 6.42
CHEMBL5597923 IC50 = 425.0 nM 6.37
CHEMBL5597539 IC50 = 457.0 nM 6.34
CHEMBL5597513 IC50 = 626.0 nM 6.20
CHEMBL5598207 IC50 = 694.0 nM 6.16
CHEMBL5598292 IC50 = 731.0 nM 6.14
CHEMBL3264002 AVUTOMETINIB IC50 = 739.0 nM 6.13
CHEMBL5598214 IC50 = 898.0 nM 6.05
CHEMBL3187723 BINIMETINIB IC50 = 1997.0 nM 5.70
CHEMBL5590964 IC50 - -
CHEMBL5597616 IC50 - -
CHEMBL5596617 IC50 - -
CHEMBL5596318 IC50 - -
CHEMBL5597679 IC50 - -
CHEMBL5598403 IC50 - -
CHEMBL5597745 IC50 - -
CHEMBL5596682 IC50 - -
CHEMBL5597128 IC50 - -
CHEMBL5598496 IC50 - -
CHEMBL5597535 IC50 - -
CHEMBL5598254 IC50 - -
CHEMBL5597695 IC50 - -
CHEMBL5597425 IC50 - -
CHEMBL5591121 IC50 - -
CHEMBL5597532 IC50 - -
CHEMBL5596352 IC50 - -
CHEMBL5596397 IC50 - -
CHEMBL5598115 IC50 - -