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

CHEMBL873740

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

Functional
Inhibitory activity against MEK-1
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.
El Abdellaoui H, Varaprasad CV, Barawkar D, Chakravarty S, Maderna A, Tam R, Chen H, Allan M, Wu JZ, Appleby T, Yan S, Zhang W, Lang S, Yao N, Hamatake R, Hong Z.
Bioorg Med Chem Lett (2006) 16 : 5561 -5566
PubMed 16934458 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 56 6.77 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263039 — — 1 7.66
CHEMBL425980 — — 1 7.52
CHEMBL214587 — — 1 7.46
CHEMBL384784 — — 1 7.43
CHEMBL437331 — — 1 7.38
CHEMBL214613 — — 1 7.38
CHEMBL214683 — — 1 7.37
CHEMBL253116 — — 1 7.35
CHEMBL214901 — — 1 7.33
CHEMBL216833 — — 1 7.33
CHEMBL216832 — — 1 7.31
CHEMBL384012 — — 1 7.27
CHEMBL216449 — — 1 7.19
CHEMBL217126 — — 1 7.16
CHEMBL385905 — — 1 7.12
CHEMBL215038 — — 1 7.11
CHEMBL217414 — — 1 7.06
CHEMBL217833 — — 1 7.02
CHEMBL214032 — — 1 7.00
CHEMBL217130 — — 1 7.00
CHEMBL383858 — — 1 6.95
CHEMBL214977 — — 1 6.93
CHEMBL216325 — — 1 6.92
CHEMBL217832 — — 1 6.91
CHEMBL215193 — — 1 6.89
CHEMBL413636 — — 1 6.89
CHEMBL217310 — — 1 6.89
CHEMBL215011 — — 1 6.89
CHEMBL265478 — — 1 6.85
CHEMBL214816 — — 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263039 — EC50 = 22.0 nM 7.66
CHEMBL425980 — EC50 = 30.0 nM 7.52
CHEMBL214587 — EC50 = 35.0 nM 7.46
CHEMBL384784 — EC50 = 37.0 nM 7.43
CHEMBL437331 — EC50 = 42.0 nM 7.38
CHEMBL214613 — EC50 = 42.0 nM 7.38
CHEMBL214683 — EC50 = 43.0 nM 7.37
CHEMBL253116 — EC50 = 45.0 nM 7.35
CHEMBL214901 — EC50 = 47.0 nM 7.33
CHEMBL216833 — EC50 = 47.0 nM 7.33
CHEMBL216832 — EC50 = 49.0 nM 7.31
CHEMBL384012 — EC50 = 54.0 nM 7.27
CHEMBL216449 — EC50 = 65.0 nM 7.19
CHEMBL217126 — EC50 = 70.0 nM 7.16
CHEMBL385905 — EC50 = 75.0 nM 7.12
CHEMBL215038 — EC50 = 78.0 nM 7.11
CHEMBL217414 — EC50 = 88.0 nM 7.06
CHEMBL217833 — EC50 = 95.0 nM 7.02
CHEMBL214032 — EC50 = 100.0 nM 7.00
CHEMBL217130 — EC50 = 100.0 nM 7.00
CHEMBL383858 — EC50 = 113.0 nM 6.95
CHEMBL214977 — EC50 = 118.0 nM 6.93
CHEMBL216325 — EC50 = 120.0 nM 6.92
CHEMBL217832 — EC50 = 123.0 nM 6.91
CHEMBL215011 — EC50 = 128.0 nM 6.89
CHEMBL413636 — EC50 = 130.0 nM 6.89
CHEMBL215193 — EC50 = 130.0 nM 6.89
CHEMBL217310 — EC50 = 130.0 nM 6.89
CHEMBL265478 — EC50 = 140.0 nM 6.85
CHEMBL214816 — EC50 = 140.0 nM 6.85
CHEMBL214752 — EC50 = 150.0 nM 6.82
CHEMBL385203 — EC50 = 200.0 nM 6.70
CHEMBL385446 — EC50 = 220.0 nM 6.66
CHEMBL424897 — EC50 = 250.0 nM 6.60
CHEMBL215012 — EC50 = 250.0 nM 6.60
CHEMBL214425 — EC50 = 260.0 nM 6.58
CHEMBL217117 — EC50 = 278.0 nM 6.56
CHEMBL214636 — EC50 = 284.0 nM 6.55
CHEMBL387184 — EC50 = 332.0 nM 6.48
CHEMBL217415 — EC50 = 330.0 nM 6.48
CHEMBL217355 — EC50 = 350.0 nM 6.46
CHEMBL217416 — EC50 = 350.0 nM 6.46
CHEMBL375609 — EC50 = 375.0 nM 6.43
CHEMBL386469 — EC50 = 444.0 nM 6.35
CHEMBL216201 — EC50 = 564.0 nM 6.25
CHEMBL386457 — EC50 = 605.0 nM 6.22
CHEMBL386230 — EC50 = 650.0 nM 6.19
CHEMBL385059 — EC50 = 694.0 nM 6.16
CHEMBL214734 — EC50 = 1450.0 nM 5.84
CHEMBL211359 — EC50 = 1480.0 nM 5.83