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Assay Detail

CHEMBL963128

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

Binding
Inhibition of MEK-mediated phosphorylation of myelin basic protein by kinase cascade assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA, Smith Y, Warmus JS, Tecle H.
Bioorg Med Chem Lett (2008) 18 : 6501 -6504
PubMed 18952427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.54 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105442 CI-1040 2.0 1 8.64
CHEMBL510244 1 8.55
CHEMBL455839 1 8.24
CHEMBL519419 1 8.17
CHEMBL453890 1 8.15
CHEMBL454114 1 8.11
CHEMBL511056 1 8.10
CHEMBL510625 1 8.00
CHEMBL455472 1 7.89
CHEMBL446522 1 7.82
CHEMBL454880 1 7.75
CHEMBL442641 1 7.70
CHEMBL454115 1 7.64
CHEMBL448323 1 7.58
CHEMBL455471 1 7.57
CHEMBL455470 1 7.46
CHEMBL454116 1 7.32
CHEMBL487237 1 6.78
CHEMBL488252 1 6.41
CHEMBL520226 1 6.29
CHEMBL488090 1 6.26
CHEMBL505548 1 5.52
CHEMBL23971 1 -
CHEMBL488253 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105442 CI-1040 IC50 = 2.3 nM 8.64
CHEMBL510244 IC50 = 2.8 nM 8.55
CHEMBL455839 IC50 = 5.8 nM 8.24
CHEMBL519419 IC50 = 6.8 nM 8.17
CHEMBL453890 IC50 = 7.0 nM 8.15
CHEMBL454114 IC50 = 7.8 nM 8.11
CHEMBL511056 IC50 = 7.96 nM 8.10
CHEMBL510625 IC50 = 10.0 nM 8.00
CHEMBL455472 IC50 = 13.0 nM 7.89
CHEMBL446522 IC50 = 15.0 nM 7.82
CHEMBL454880 IC50 = 18.0 nM 7.75
CHEMBL442641 IC50 = 20.0 nM 7.70
CHEMBL454115 IC50 = 23.0 nM 7.64
CHEMBL448323 IC50 = 26.0 nM 7.58
CHEMBL455471 IC50 = 27.0 nM 7.57
CHEMBL455470 IC50 = 35.0 nM 7.46
CHEMBL454116 IC50 = 48.0 nM 7.32
CHEMBL487237 IC50 = 166.0 nM 6.78
CHEMBL488252 IC50 = 390.0 nM 6.41
CHEMBL520226 IC50 = 518.0 nM 6.29
CHEMBL488090 IC50 = 554.0 nM 6.26
CHEMBL505548 IC50 = 3050.0 nM 5.52
CHEMBL23971 IC50 > 10000.0 nM -
CHEMBL488253 IC50 > 10000.0 nM -