Assay Detail

CHEMBL1685627

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Binding

Binding affinity to MEK1 by surface plasmon resonance in absence of ATP

ChEMBL ↗

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Target

Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗

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Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Dual specificity mitogen-activated protein kinase kinase 1

CHEMBL3587

Anchored from Assay target.

Protein identity Dual specificity mitogen-activated protein kinase kinase 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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
Kd	2	7.79	8.06

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1614766	RO-4987655	1.0	1	8.06
CHEMBL507361	MIRDAMETINIB	2.0	1	7.51

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1614766	RO-4987655	Kd	=	8.7	nM	8.06
CHEMBL507361	MIRDAMETINIB	Kd	=	31.0	nM	7.51