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Assay Detail

CHEMBL1787945

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

Binding
Inhibition of PYK2 by PYK2-LI-COR cellular assay
13
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein-tyrosine kinase 2-beta (CHEMBL5469)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity.
Walker DP, Zawistoski MP, McGlynn MA, Li JC, Kung DW, Bonnette PC, Baumann A, Buckbinder L, Houser JA, Boer J, Mistry A, Han S, Xing L, Guzman-Perez A.
Bioorg Med Chem Lett (2009) 19 : 3253 -3258
PubMed 19428251 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.30 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2029181 3 8.00
CHEMBL2448536 1 7.62
CHEMBL2029180 3 7.54
CHEMBL2029182 1 7.47
CHEMBL519418 1 7.22
CHEMBL472212 1 7.20
CHEMBL509485 1 7.06
CHEMBL1783837 1 7.02
CHEMBL2029183 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2029181 IC50 = 10.0 nM 8.00
CHEMBL2029181 IC50 = 22.0 nM 7.66
CHEMBL2448536 IC50 = 24.0 nM 7.62
CHEMBL2029180 IC50 = 29.0 nM 7.54
CHEMBL2029182 IC50 = 34.0 nM 7.47
CHEMBL2029181 IC50 = 37.0 nM 7.43
CHEMBL519418 IC50 = 60.0 nM 7.22
CHEMBL472212 IC50 = 63.0 nM 7.20
CHEMBL2029180 IC50 = 76.0 nM 7.12
CHEMBL509485 IC50 = 88.0 nM 7.06
CHEMBL1783837 IC50 = 95.0 nM 7.02
CHEMBL2029180 IC50 = 98.0 nM 7.01
CHEMBL2029183 IC50 = 320.0 nM 6.50