Assay Detail

CHEMBL5716867

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Binding

Inhibition of GST-fused His-tagged recombinant FAK KD (411 to 686 residues) (unknown origin) expressed in baculovirus infected Sf9 cells using poly(Glu:Tyr) as substrate in presence of ATP by coomassie blue staining based ELISA screening assay

ChEMBL ↗

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Target

Focal adhesion kinase 1 (CHEMBL2695) ↗

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Focal adhesion kinase 1 (CHEMBL2695) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Focal adhesion kinase 1

CHEMBL2695

Anchored from Assay target.

Protein identity Focal adhesion 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
Organism	Homo sapiens
Cell Type	Sf9
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Focal adhesion kinase 1 (CHEMBL2695) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments.

Tanjoni I, Walsh C, Uryu S, Tomar A, Nam JO, Mielgo A, Lim ST, Liang C, Koenig M, Sun C, Patel N, Kwok C, McMahon G, Stupack DG, Schlaepfer DD.
Cancer Biol Ther (2010) 9 : 764 -777
PubMed 20234191 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.82	8.82

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_TERM	EFO_TERM	-	—	cancer

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3040440	VS-4718	1.0	1	8.82

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3040440	VS-4718	IC50	=	1.5	nM	8.82