Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5127375

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

Binding
Inhibition of mouse recombinant GST-fused CLK2 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity protein kinase CLK2 (CHEMBL1075281) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.
Tahtouh T, Durieu E, Villiers B, Bruyère C, Nguyen TL, Fant X, Ahn KH, Khurana L, Deau E, Lindberg MF, Sévère E, Miege F, Roche D, Limanton E, L'Helgoual'ch JM, Burgy G, Guiheneuf S, Herault Y, Kendall DA, Carreaux F, Bazureau JP, Meijer L.
J Med Chem (2022) 65 : 1396 -1417
PubMed 34928152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.28 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5200518 — — 1 7.52
CHEMBL5179655 — — 1 7.46
CHEMBL5195216 — — 1 7.17
CHEMBL1803085 — — 1 7.08
CHEMBL5206143 — — 1 6.96
CHEMBL5181355 — — 1 6.92
CHEMBL5208980 — — 1 6.92
CHEMBL5181008 — — 1 6.92
CHEMBL5196066 — — 1 6.89
CHEMBL1802358 — — 1 6.89
CHEMBL5195122 — — 1 6.85
CHEMBL5199422 — — 1 6.77
CHEMBL5203292 — — 1 6.75
CHEMBL5179457 — — 1 6.75
CHEMBL5206744 — — 1 6.66
CHEMBL5187753 — — 1 6.60
CHEMBL5180765 — — 1 6.58
CHEMBL5194491 — — 1 6.50
CHEMBL1803082 — — 1 6.42
CHEMBL5187895 — — 1 6.38
CHEMBL1803069 — — 1 6.30
CHEMBL5200677 — — 1 6.28
CHEMBL1803079 — — 1 6.26
CHEMBL1802843 — — 1 6.25
CHEMBL5194689 — — 1 6.06
CHEMBL5193677 — — 1 6.05
CHEMBL485053 LEUCETTAMINE B — 1 6.03
CHEMBL1803084 — — 1 6.00
CHEMBL5170033 — — 1 5.96
CHEMBL5182235 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5200518 — IC50 = 30.0 nM 7.52
CHEMBL5179655 — IC50 = 35.0 nM 7.46
CHEMBL5195216 — IC50 = 67.0 nM 7.17
CHEMBL1803085 — IC50 = 83.0 nM 7.08
CHEMBL5206143 — IC50 = 110.0 nM 6.96
CHEMBL5181355 — IC50 = 120.0 nM 6.92
CHEMBL5208980 — IC50 = 120.0 nM 6.92
CHEMBL5181008 — IC50 = 120.0 nM 6.92
CHEMBL5196066 — IC50 = 130.0 nM 6.89
CHEMBL1802358 — IC50 = 130.0 nM 6.89
CHEMBL5195122 — IC50 = 140.0 nM 6.85
CHEMBL5199422 — IC50 = 170.0 nM 6.77
CHEMBL5203292 — IC50 = 180.0 nM 6.75
CHEMBL5179457 — IC50 = 180.0 nM 6.75
CHEMBL5206744 — IC50 = 220.0 nM 6.66
CHEMBL5187753 — IC50 = 250.0 nM 6.60
CHEMBL5180765 — IC50 = 260.0 nM 6.58
CHEMBL5194491 — IC50 = 320.0 nM 6.50
CHEMBL1803082 — IC50 = 380.0 nM 6.42
CHEMBL5187895 — IC50 = 420.0 nM 6.38
CHEMBL1803069 — IC50 = 500.0 nM 6.30
CHEMBL5200677 — IC50 = 530.0 nM 6.28
CHEMBL1803079 — IC50 = 550.0 nM 6.26
CHEMBL1802843 — IC50 = 560.0 nM 6.25
CHEMBL5194689 — IC50 = 880.0 nM 6.06
CHEMBL5193677 — IC50 = 900.0 nM 6.05
CHEMBL485053 LEUCETTAMINE B IC50 = 940.0 nM 6.03
CHEMBL1803084 — IC50 = 1000.0 nM 6.00
CHEMBL5170033 — IC50 = 1100.0 nM 5.96
CHEMBL5182235 — IC50 = 1200.0 nM 5.92
CHEMBL5201763 — IC50 = 1300.0 nM 5.89
CHEMBL5207630 — IC50 = 1500.0 nM 5.82
CHEMBL5191942 — IC50 = 1500.0 nM 5.82
CHEMBL5202202 — IC50 = 1800.0 nM 5.75
CHEMBL5207974 — IC50 = 1800.0 nM 5.75
CHEMBL5172170 — IC50 = 2200.0 nM 5.66
CHEMBL5175458 — IC50 = 2300.0 nM 5.64
CHEMBL5173265 — IC50 = 2300.0 nM 5.64
CHEMBL1803081 — IC50 = 2500.0 nM 5.60
CHEMBL5209464 — IC50 = 3100.0 nM 5.51
CHEMBL5172199 — IC50 = 3200.0 nM 5.50
CHEMBL5205905 — IC50 = 3500.0 nM 5.46
CHEMBL1802355 — IC50 = 7500.0 nM 5.12
CHEMBL5187202 — IC50 = 10000.0 nM 5.00
CHEMBL5169649 — IC50 > 10000.0 nM -
CHEMBL5205157 — IC50 > 10000.0 nM -
CHEMBL5179916 — IC50 >= 10000.0 nM -
CHEMBL5177952 — IC50 > 10000.0 nM -
CHEMBL5176573 — IC50 > 10000.0 nM -
CHEMBL5188100 — IC50 > 10000.0 nM -