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Assay Detail

CHEMBL1686838

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

Functional
Cytotoxicity against human COLO205 cells after 72 hrs by MTS assay
17
Total Activities
17
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 Autocuration

Target

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

Publication

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.
Dong Q, Dougan DR, Gong X, Halkowycz P, Jin B, Kanouni T, O'Connell SM, Scorah N, Shi L, Wallace MB, Zhou F.
Bioorg Med Chem Lett (2011) 21 : 1315 -1319
PubMed 21310613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684075 1 9.00
CHEMBL1615025 TAK-733 2.0 1 8.68
CHEMBL1684070 1 8.59
CHEMBL1684074 1 8.46
CHEMBL1684072 1 8.43
CHEMBL1684067 1 8.10
CHEMBL1684073 1 8.05
CHEMBL1684069 1 8.00
CHEMBL1681812 1 8.00
CHEMBL1684071 1 7.89
CHEMBL1684062 1 7.80
CHEMBL1684063 1 7.57
CHEMBL1684064 1 7.42
CHEMBL1684068 1 7.42
CHEMBL1684061 1 7.42
CHEMBL1684060 1 7.31
CHEMBL1684065 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684075 EC50 = 1.0 nM 9.00
CHEMBL1615025 TAK-733 EC50 = 2.1 nM 8.68
CHEMBL1684070 EC50 = 2.6 nM 8.59
CHEMBL1684074 EC50 = 3.5 nM 8.46
CHEMBL1684072 EC50 = 3.7 nM 8.43
CHEMBL1684067 EC50 = 7.9 nM 8.10
CHEMBL1684073 EC50 = 9.0 nM 8.05
CHEMBL1684069 EC50 = 10.0 nM 8.00
CHEMBL1681812 EC50 = 10.0 nM 8.00
CHEMBL1684071 EC50 = 13.0 nM 7.89
CHEMBL1684062 EC50 = 16.0 nM 7.80
CHEMBL1684063 EC50 = 27.0 nM 7.57
CHEMBL1684064 EC50 = 38.0 nM 7.42
CHEMBL1684068 EC50 = 38.0 nM 7.42
CHEMBL1684061 EC50 = 38.0 nM 7.42
CHEMBL1684060 EC50 = 49.0 nM 7.31
CHEMBL1684065 EC50 = 142.0 nM 6.85