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Assay Detail

CHEMBL3705339

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

Binding
Enzymatic Assay: The enzymatic activity of PAK4 KD was measured by its ability to catalyzed the transfer of a phosphate residue from a nucleoside triphosphate to an amino acid side chain of a commercially available peptide (amino acid sequence EVPRRKSLVGTPYWM).
ChEMBL ↗
145
Total Activities
82
Compounds Tested
2
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

Pyrrolopyrazoles, potent kinase inhibitors
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 82 7.16 8.80
EC50 63 7.12 9.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3669583 — — 2 9.03
CHEMBL3674597 — — 2 8.80
CHEMBL3674593 — — 2 8.72
CHEMBL3674594 — — 2 8.72
CHEMBL3669628 — — 2 8.62
CHEMBL3669627 — — 3 8.60
CHEMBL3669632 — — 2 8.52
CHEMBL3664542 — — 4 8.46
CHEMBL3674598 — — 2 8.44
CHEMBL3674596 — — 2 8.36
CHEMBL3674599 — — 2 8.28
CHEMBL3674595 — — 1 8.28
CHEMBL3669636 — — 2 8.17
CHEMBL3669607 — — 4 8.14
CHEMBL3674600 — — 2 8.08
CHEMBL3669580 — — 2 7.96
CHEMBL3669579 — — 2 7.85
CHEMBL3669631 — — 2 7.82
CHEMBL3669616 — — 4 7.80
CHEMBL3669614 — — 2 7.75
CHEMBL3669623 — — 2 7.75
CHEMBL3669630 — — 2 7.72
CHEMBL3128043 PF-03758309 1.0 2 7.70
CHEMBL3669635 — — 2 7.70
CHEMBL3674604 — — 2 7.70
CHEMBL3669608 — — 2 7.68
CHEMBL3669615 — — 2 7.62
CHEMBL3669619 — — 2 7.60
CHEMBL3674609 — — 2 7.47
CHEMBL3669589 — — 2 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3669583 — EC50 = 0.94 nM 9.03
CHEMBL3674597 — Ki = 1.6 nM 8.80
CHEMBL3674593 — Ki = 1.9 nM 8.72
CHEMBL3674594 — EC50 = 1.9 nM 8.72
CHEMBL3669628 — EC50 = 2.4 nM 8.62
CHEMBL3669627 — EC50 = 2.5 nM 8.60
CHEMBL3669583 — Ki = 2.8 nM 8.55
CHEMBL3674593 — EC50 = 3.0 nM 8.52
CHEMBL3669632 — Ki = 3.0 nM 8.52
CHEMBL3664542 — Ki = 3.5 nM 8.46
CHEMBL3664542 — Ki = 3.5 nM 8.46
CHEMBL3674598 — Ki = 3.6 nM 8.44
CHEMBL3674596 — EC50 = 4.4 nM 8.36
CHEMBL3674595 — Ki = 5.2 nM 8.28
CHEMBL3674599 — Ki = 5.2 nM 8.28
CHEMBL3669636 — Ki = 6.7 nM 8.17
CHEMBL3669607 — Ki = 7.2 nM 8.14
CHEMBL3674600 — Ki = 8.3 nM 8.08
CHEMBL3674594 — Ki = 8.8 nM 8.06
CHEMBL3669580 — Ki = 11.0 nM 7.96
CHEMBL3669579 — Ki = 14.0 nM 7.85
CHEMBL3669627 — Ki = 14.0 nM 7.85
CHEMBL3669631 — EC50 = 15.0 nM 7.82
CHEMBL3669631 — Ki = 15.0 nM 7.82
CHEMBL3669616 — Ki = 16.0 nM 7.80
CHEMBL3674596 — Ki = 16.0 nM 7.80
CHEMBL3669580 — EC50 = 16.0 nM 7.80
CHEMBL3669623 — Ki = 18.0 nM 7.75
CHEMBL3669614 — Ki = 18.0 nM 7.75
CHEMBL3664542 — EC50 = 19.0 nM 7.72
CHEMBL3669630 — EC50 = 19.0 nM 7.72
CHEMBL3664542 — EC50 = 19.0 nM 7.72
CHEMBL3674604 — EC50 = 20.0 nM 7.70
CHEMBL3669636 — EC50 = 20.0 nM 7.70
CHEMBL3669635 — EC50 = 20.0 nM 7.70
CHEMBL3128043 PF-03758309 Ki = 20.0 nM 7.70
CHEMBL3669607 — Ki = 20.0 nM 7.70
CHEMBL3669608 — Ki = 21.0 nM 7.68
CHEMBL3669607 — EC50 = 21.0 nM 7.68
CHEMBL3669630 — Ki = 22.0 nM 7.66
CHEMBL3669615 — Ki = 24.0 nM 7.62
CHEMBL3669619 — Ki = 25.0 nM 7.60
CHEMBL3669623 — EC50 = 31.0 nM 7.51
CHEMBL3669619 — EC50 = 32.0 nM 7.50
CHEMBL3674609 — Ki = 34.0 nM 7.47
CHEMBL3669579 — EC50 = 36.0 nM 7.44
CHEMBL3669589 — Ki = 38.0 nM 7.42
CHEMBL3674603 — Ki = 39.0 nM 7.41
CHEMBL3669629 — Ki = 40.0 nM 7.40
CHEMBL3674607 — Ki = 41.0 nM 7.39