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Assay Detail

CHEMBL1685467

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

Binding
Inhibition of MEK after 30 mins
14
Total Activities
14
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

Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent.
Isshiki Y, Kohchi Y, Iikura H, Matsubara Y, Asoh K, Murata T, Kohchi M, Mizuguchi E, Tsujii S, Hattori K, Miura T, Yoshimura Y, Aida S, Miwa M, Saitoh R, Murao N, Okabe H, Belunis C, Janson C, Lukacs C, Schück V, Shimma N.
Bioorg Med Chem Lett (2011) 21 : 1795 -1801
PubMed 21316218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.53 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1614766 RO-4987655 1.0 1 8.28
CHEMBL1684493 1 8.14
CHEMBL1684492 1 8.07
CHEMBL464238 1 7.85
CHEMBL1684490 1 7.82
CHEMBL1684491 1 7.72
CHEMBL1684487 1 7.43
CHEMBL1684496 1 7.38
CHEMBL1684489 1 7.32
CHEMBL1684488 1 7.17
CHEMBL1684494 1 7.07
CHEMBL464239 1 7.00
CHEMBL1684486 1 6.63
CHEMBL1684495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1614766 RO-4987655 IC50 = 5.2 nM 8.28
CHEMBL1684493 IC50 = 7.2 nM 8.14
CHEMBL1684492 IC50 = 8.6 nM 8.07
CHEMBL464238 IC50 = 14.0 nM 7.85
CHEMBL1684490 IC50 = 15.0 nM 7.82
CHEMBL1684491 IC50 = 19.0 nM 7.72
CHEMBL1684487 IC50 = 37.0 nM 7.43
CHEMBL1684496 IC50 = 42.0 nM 7.38
CHEMBL1684489 IC50 = 48.0 nM 7.32
CHEMBL1684488 IC50 = 67.0 nM 7.17
CHEMBL1684494 IC50 = 85.0 nM 7.07
CHEMBL464239 IC50 = 100.0 nM 7.00
CHEMBL1684486 IC50 = 235.0 nM 6.63
CHEMBL1684495 IC50 > 250.0 nM -