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Assay Detail

CHEMBL4033369

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

Binding
Binding affinity to biotin-labeled human truncated PAK4 kinase domain by surface plasmon resonance assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase PAK 4 (CHEMBL4482)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.
Hao C, Zhao F, Song H, Guo J, Li X, Jiang X, Huan R, Song S, Zhang Q, Wang R, Wang K, Pang Y, Liu T, Lu T, Huang W, Wang J, Lin B, He Z, Li H, Li F, Zhao D, Cheng M.
J Med Chem (2018) 61 : 265 -285
PubMed 29190083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.18 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4076708 1 8.22
CHEMBL4064068 1 7.80
CHEMBL4091048 1 7.37
CHEMBL4093999 1 7.18
CHEMBL4084054 1 6.81
CHEMBL4093649 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4076708 Kd = 6.0 nM 8.22
CHEMBL4064068 Kd = 16.0 nM 7.80
CHEMBL4091048 Kd = 43.0 nM 7.37
CHEMBL4093999 Kd = 66.0 nM 7.18
CHEMBL4084054 Kd = 156.0 nM 6.81
CHEMBL4093649 Kd = 1940.0 nM 5.71