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Assay Detail

CHEMBL5111624

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

Binding
Inhibition of recombinant full length LIMK2 (330 to 632 residues) (unknown origin) expressed in HEK293T cells incubated for 2 hrs in presence of tracer K10 by NanoBRET assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

LIM domain kinase 2 (CHEMBL5932)
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 17 6.86 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5169387 1 7.89
CHEMBL2141887 1 7.77
CHEMBL5181311 1 7.21
CHEMBL5206269 1 7.19
CHEMBL5190928 1 7.17
CHEMBL5184302 1 7.06
CHEMBL5184275 1 7.05
CHEMBL4790618 1 7.04
CHEMBL5179261 1 7.04
CHEMBL5190028 1 6.93
CHEMBL5202731 1 6.92
CHEMBL5192852 1 6.79
CHEMBL5184915 1 6.49
CHEMBL5180888 1 6.36
CHEMBL5180550 1 6.24
CHEMBL5174511 1 4.62
CHEMBL4779405 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5169387 IC50 = 13.0 nM 7.89
CHEMBL2141887 IC50 = 17.0 nM 7.77
CHEMBL5181311 IC50 = 61.0 nM 7.21
CHEMBL5206269 IC50 = 65.0 nM 7.19
CHEMBL5190928 IC50 = 67.0 nM 7.17
CHEMBL5184302 IC50 = 87.0 nM 7.06
CHEMBL5184275 IC50 = 90.0 nM 7.05
CHEMBL4790618 IC50 = 91.0 nM 7.04
CHEMBL5179261 IC50 = 92.0 nM 7.04
CHEMBL5190028 IC50 = 118.0 nM 6.93
CHEMBL5202731 IC50 = 121.0 nM 6.92
CHEMBL5192852 IC50 = 161.0 nM 6.79
CHEMBL5184915 IC50 = 323.0 nM 6.49
CHEMBL5180888 IC50 = 440.0 nM 6.36
CHEMBL5180550 IC50 = 573.0 nM 6.24
CHEMBL5174511 IC50 = 23900.0 nM 4.62
CHEMBL4779405 IC50 > 25000.0 nM -