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Assay Detail

CHEMBL960615

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

Binding
Inhibition of GST-tagged FAK assessed as inhibition of poly-Glu-Tyr phosphorylation by fluorescence polarization assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Focal adhesion kinase 1 (CHEMBL2695)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Walker DP, Bi FC, Kalgutkar AS, Bauman JN, Zhao SX, Soglia JR, Aspnes GE, Kung DW, Klug-McLeod J, Zawistoski MP, McGlynn MA, Oliver R, Dunn M, Li JC, Richter DT, Cooper BA, Kath JC, Hulford CA, Autry CL, Luzzio MJ, Ung EJ, Roberts WG, Bonnette PC, Buckbinder L, Mistry A, Griffor MC, Han S, Guzman-Perez A.
Bioorg Med Chem Lett (2008) 18 : 6071 -6077
PubMed 18951788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.30 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL453649 1 5.40
CHEMBL509485 1 5.35
CHEMBL452340 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL453649 IC50 = 4000.0 nM 5.40
CHEMBL509485 IC50 = 4500.0 nM 5.35
CHEMBL452340 IC50 = 6900.0 nM 5.16