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Assay Detail

CHEMBL5588078

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Functional
Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant incubated for 72 hrs by CCK8 assay
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

MIA PaCa-2 (CHEMBL614725) ↗
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 6.86 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5597316 — — 1 7.96
CHEMBL5597799 — — 1 7.82
CHEMBL5596257 — — 1 7.64
CHEMBL5598292 — — 1 7.51
CHEMBL5596481 — — 1 7.50
CHEMBL5596544 — — 1 7.37
CHEMBL5596447 — — 1 7.33
CHEMBL5597923 — — 1 7.32
CHEMBL5596121 — — 1 7.22
CHEMBL5596553 — — 1 7.15
CHEMBL3264002 AVUTOMETINIB 3.0 1 6.94
CHEMBL5597586 — — 1 6.94
CHEMBL5598512 — — 1 6.90
CHEMBL5597695 — — 1 6.86
CHEMBL5598180 — — 1 6.82
CHEMBL5597513 — — 1 6.77
CHEMBL3187723 BINIMETINIB 4.0 1 6.74
CHEMBL5597539 — — 1 6.66
CHEMBL5597470 — — 1 6.65
CHEMBL5591121 — — 1 6.62
CHEMBL5598214 — — 1 6.60
CHEMBL5596979 — — 1 6.44
CHEMBL5598403 — — 1 6.21
CHEMBL5598254 — — 1 6.20
CHEMBL5598207 — — 1 6.07
CHEMBL5597532 — — 1 6.03
CHEMBL5597425 — — 1 6.01
CHEMBL5597535 — — 1 5.89
CHEMBL5596617 — — 1 -
CHEMBL5597128 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5597316 — IC50 = 11.0 nM 7.96
CHEMBL5597799 — IC50 = 15.0 nM 7.82
CHEMBL5596257 — IC50 = 23.0 nM 7.64
CHEMBL5598292 — IC50 = 31.0 nM 7.51
CHEMBL5596481 — IC50 = 32.0 nM 7.50
CHEMBL5596544 — IC50 = 43.0 nM 7.37
CHEMBL5596447 — IC50 = 47.0 nM 7.33
CHEMBL5597923 — IC50 = 48.0 nM 7.32
CHEMBL5596121 — IC50 = 60.0 nM 7.22
CHEMBL5596553 — IC50 = 71.0 nM 7.15
CHEMBL5597586 — IC50 = 114.0 nM 6.94
CHEMBL3264002 AVUTOMETINIB IC50 = 115.0 nM 6.94
CHEMBL5598512 — IC50 = 127.0 nM 6.90
CHEMBL5597695 — IC50 = 138.0 nM 6.86
CHEMBL5598180 — IC50 = 150.0 nM 6.82
CHEMBL5597513 — IC50 = 169.0 nM 6.77
CHEMBL3187723 BINIMETINIB IC50 = 182.0 nM 6.74
CHEMBL5597539 — IC50 = 219.0 nM 6.66
CHEMBL5597470 — IC50 = 225.0 nM 6.65
CHEMBL5591121 — IC50 = 237.0 nM 6.62
CHEMBL5598214 — IC50 = 249.0 nM 6.60
CHEMBL5596979 — IC50 = 362.0 nM 6.44
CHEMBL5598403 — IC50 = 611.0 nM 6.21
CHEMBL5598254 — IC50 = 628.0 nM 6.20
CHEMBL5598207 — IC50 = 861.0 nM 6.07
CHEMBL5597532 — IC50 = 942.0 nM 6.03
CHEMBL5597425 — IC50 = 985.0 nM 6.01
CHEMBL5597535 — IC50 = 1275.0 nM 5.89
CHEMBL5598115 — IC50 - — -
CHEMBL5597616 — IC50 - — -
CHEMBL5596397 — IC50 - — -
CHEMBL5596352 — IC50 - — -
CHEMBL5590964 — IC50 - — -
CHEMBL5597745 — IC50 - — -
CHEMBL5598496 — IC50 - — -
CHEMBL5596318 — IC50 - — -
CHEMBL5597679 — IC50 - — -
CHEMBL5596682 — IC50 - — -
CHEMBL5597128 — IC50 - — -
CHEMBL5596617 — IC50 - — -