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Assay Detail

CHEMBL3090922

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

Functional
Growth inhibition of human HCT116 cells after 96 hrs by CCK-8 assay
17
Total Activities
17
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

The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ori K, Takanashi K, Harada N, Tomii Y, Tabo M, Yoshinari K, Aoki Y, Shimma N, Iikura H.
Bioorg Med Chem Lett (2013) 23 : 6223 -6227
PubMed 24157370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.13 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3086065 1 8.40
CHEMBL3086078 1 8.10
CHEMBL3086066 1 7.92
CHEMBL3086073 1 7.64
CHEMBL3086068 1 7.52
CHEMBL3086075 1 7.44
CHEMBL3086069 1 7.44
CHEMBL3086064 1 7.41
CHEMBL3086074 1 7.38
CHEMBL3086071 1 7.17
CHEMBL3086072 1 7.03
CHEMBL3086076 1 6.80
CHEMBL3086070 1 6.77
CHEMBL3086063 1 6.54
CHEMBL81277 1 6.44
CHEMBL3086062 1 5.92
CHEMBL3086067 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3086065 IC50 = 4.0 nM 8.40
CHEMBL3086078 IC50 = 8.0 nM 8.10
CHEMBL3086066 IC50 = 12.0 nM 7.92
CHEMBL3086073 IC50 = 23.0 nM 7.64
CHEMBL3086068 IC50 = 30.0 nM 7.52
CHEMBL3086075 IC50 = 36.0 nM 7.44
CHEMBL3086069 IC50 = 36.0 nM 7.44
CHEMBL3086064 IC50 = 39.0 nM 7.41
CHEMBL3086074 IC50 = 42.0 nM 7.38
CHEMBL3086071 IC50 = 68.0 nM 7.17
CHEMBL3086072 IC50 = 93.0 nM 7.03
CHEMBL3086076 IC50 = 160.0 nM 6.80
CHEMBL3086070 IC50 = 170.0 nM 6.77
CHEMBL3086063 IC50 = 290.0 nM 6.54
CHEMBL81277 IC50 = 360.0 nM 6.44
CHEMBL3086062 IC50 = 1200.0 nM 5.92
CHEMBL3086067 IC50 = 4600.0 nM 5.34