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Assay Detail

CHEMBL5112349

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

Binding
Inhibition of recombinant LIMK2 (347 to 659 residues) (unknown origin) incubated for 45 mins followed by ATP addition measured after 180 mins by RapidFire Mass Spectrometry kinase assay
21
Total Activities
21
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 2 (CHEMBL5932)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
Collins R, Lee H, Jones DH, Elkins JM, Gillespie JA, Thomas C, Baldwin AG, Jones K, Waters L, Paine M, Atack JR, Ward SE, Grubisha O, Foley DW.
J Med Chem (2022) 65 : 13705 -13713
PubMed 36205722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.29 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570116 1 8.74
CHEMBL5169387 1 8.26
CHEMBL5202859 1 8.20
CHEMBL3355509 1 8.14
CHEMBL3356433 LX-7101 1.0 1 7.97
CHEMBL3355507 1 7.90
CHEMBL3609326 1 7.87
CHEMBL4790618 1 7.84
CHEMBL3182065 1 7.52
CHEMBL2141887 1 7.48
CHEMBL5186508 1 7.40
CHEMBL2070615 1 6.87
CHEMBL5416410 DASATINIB 4.0 1 6.65
CHEMBL3355491 1 6.57
CHEMBL3410036 1 5.72
CHEMBL1774055 1 5.71
CHEMBL363160 PHA-680632 1 5.10
CHEMBL2107823 GANDOTINIB 2.0 1 -
CHEMBL3185148 1 -
CHEMBL3990456 1 -
CHEMBL4303259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570116 IC50 = 1.82 nM 8.74
CHEMBL5169387 IC50 = 5.495 nM 8.26
CHEMBL5202859 IC50 = 6.31 nM 8.20
CHEMBL3355509 IC50 = 7.244 nM 8.14
CHEMBL3356433 LX-7101 IC50 = 10.72 nM 7.97
CHEMBL3355507 IC50 = 12.59 nM 7.90
CHEMBL3609326 IC50 = 13.49 nM 7.87
CHEMBL4790618 IC50 = 14.45 nM 7.84
CHEMBL3182065 IC50 = 30.2 nM 7.52
CHEMBL2141887 IC50 = 33.11 nM 7.48
CHEMBL5186508 IC50 = 39.81 nM 7.40
CHEMBL2070615 IC50 = 134.9 nM 6.87
CHEMBL5416410 DASATINIB IC50 = 223.87 nM 6.65
CHEMBL3355491 IC50 = 269.15 nM 6.57
CHEMBL3410036 IC50 = 1905.46 nM 5.72
CHEMBL1774055 IC50 = 1949.84 nM 5.71
CHEMBL363160 PHA-680632 IC50 = 7943.28 nM 5.10
CHEMBL2107823 GANDOTINIB IC50 > 10000.0 nM -
CHEMBL3185148 IC50 > 10000.0 nM -
CHEMBL3990456 IC50 > 10000.0 nM -
CHEMBL4303259 IC50 > 10000.0 nM -