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Assay Detail

CHEMBL5111625

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

Binding
Inhibition of recombinant LIMK1 (330 to 637 residues) (unknown origin) expressed in baculovirus infected insect cells using CFL1 as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by RapidFire mass spectrometry
4
Total Activities
4
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

LIM domain kinase 1 (CHEMBL3836)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.
Hanke T, Mathea S, Woortman J, Salah E, Berger BT, Tumber A, Kashima R, Hata A, Kuster B, Müller S, Knapp S.
J Med Chem (2022) 65 : 13264 -13287
PubMed 36136092 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.67 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5169387 1 8.15
CHEMBL2141887 1 7.78
CHEMBL4790618 1 7.08
CHEMBL4779405 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5169387 IC50 = 7.0 nM 8.15
CHEMBL2141887 IC50 = 16.6 nM 7.78
CHEMBL4790618 IC50 = 83.8 nM 7.08
CHEMBL4779405 IC50 > 50000.0 nM -