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Assay Detail

CHEMBL3624101

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

Binding
Inhibition of LIMK1 in human ZR75-1 cells assessed as inhibition of cofilin phosphorylation after 5 hrs
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type ZR-75-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties.
Charles MD, Brookfield JL, Ekwuru TC, Stockley M, Dunn J, Riddick M, Hammonds T, Trivier E, Greenland G, Wong AC, Cheasty A, Boyd S, Crighton D, Olson MF.
J Med Chem (2015) 58 : 8309 -8313
PubMed 26356364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.54 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3623438 1 6.22
CHEMBL3623441 1 6.10
CHEMBL3623440 1 5.85
CHEMBL3623435 1 5.82
CHEMBL3623443 1 5.70
CHEMBL3623437 1 5.68
CHEMBL3622873 1 5.66
CHEMBL3622874 1 5.60
CHEMBL3622867 1 5.42
CHEMBL3623439 1 5.18
CHEMBL3623436 1 5.04
CHEMBL3622871 1 4.94
CHEMBL3623434 1 4.85
CHEMBL3623433 1 -
CHEMBL3622875 1 -
CHEMBL3622872 1 -
CHEMBL3622870 1 -
CHEMBL3622869 1 -
CHEMBL3623442 1 -
CHEMBL3622868 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3623438 IC50 = 600.0 nM 6.22
CHEMBL3623441 IC50 = 800.0 nM 6.10
CHEMBL3623440 IC50 = 1400.0 nM 5.85
CHEMBL3623435 IC50 = 1500.0 nM 5.82
CHEMBL3623443 IC50 = 2000.0 nM 5.70
CHEMBL3623437 IC50 = 2100.0 nM 5.68
CHEMBL3622873 IC50 = 2200.0 nM 5.66
CHEMBL3622874 IC50 = 2500.0 nM 5.60
CHEMBL3622867 IC50 = 3800.0 nM 5.42
CHEMBL3623439 IC50 = 6600.0 nM 5.18
CHEMBL3623436 IC50 = 9200.0 nM 5.04
CHEMBL3622871 IC50 = 11500.0 nM 4.94
CHEMBL3623434 IC50 = 14000.0 nM 4.85
CHEMBL3623433 IC50 - -
CHEMBL3622875 IC50 > 30000.0 nM -
CHEMBL3622872 IC50 - -
CHEMBL3622870 IC50 - -
CHEMBL3622869 IC50 - -
CHEMBL3623442 IC50 - -
CHEMBL3622868 IC50 - -