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Assay Detail

CHEMBL3801111

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

Binding
Inhibition of human LIMK2 using cofilin as substrate preincubated for 20 mins followed by [gamma-33P]-ATP/10 uM ATP addition measured after 120 mins by radiometric assay
ChEMBL ↗
47
Total Activities
47
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

Tetrahydro-pyrimido-indoles as selective LIMK inhibitors: synthesis, selectivity profiling and structureactivity studies
Alen J, Bourin A, Boland S, Geraets J, Schroeders P, Defert O
Medchemcomm (2016) 7 : 478 -483
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 8.52 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3800458 — — 1 10.00
CHEMBL3799318 — — 1 10.00
CHEMBL3799270 — — 1 9.70
CHEMBL3798662 — — 1 9.70
CHEMBL3800259 — — 1 9.70
CHEMBL3798142 — — 1 9.70
CHEMBL3800357 — — 1 9.52
CHEMBL3799925 — — 1 9.52
CHEMBL3799236 — — 1 9.40
CHEMBL3797658 — — 1 9.40
CHEMBL3800330 — — 1 9.40
CHEMBL3797874 — — 1 9.15
CHEMBL3797519 — — 1 9.15
CHEMBL3800144 — — 1 9.10
CHEMBL3797634 — — 1 9.05
CHEMBL3799695 — — 1 9.05
CHEMBL3797469 — — 1 9.00
CHEMBL3799326 — — 1 8.85
CHEMBL3800261 — — 1 8.85
CHEMBL3356433 LX-7101 1.0 1 8.80
CHEMBL3800273 — — 1 8.70
CHEMBL3798406 — — 1 8.43
CHEMBL3800104 — — 1 8.35
CHEMBL3798086 — — 1 8.32
CHEMBL3800515 — — 1 8.15
CHEMBL3798226 — — 1 7.96
CHEMBL3799312 — — 1 7.92
CHEMBL3797875 — — 1 7.92
CHEMBL3797333 — — 1 7.89
CHEMBL3798698 — — 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3800458 — IC50 = 0.1 nM 10.00
CHEMBL3799318 — IC50 = 0.1 nM 10.00
CHEMBL3798662 — IC50 = 0.2 nM 9.70
CHEMBL3800259 — IC50 = 0.2 nM 9.70
CHEMBL3798142 — IC50 = 0.2 nM 9.70
CHEMBL3799270 — IC50 = 0.2 nM 9.70
CHEMBL3800357 — IC50 = 0.3 nM 9.52
CHEMBL3799925 — IC50 = 0.3 nM 9.52
CHEMBL3799236 — IC50 = 0.4 nM 9.40
CHEMBL3797658 — IC50 = 0.4 nM 9.40
CHEMBL3800330 — IC50 = 0.4 nM 9.40
CHEMBL3797874 — IC50 = 0.7 nM 9.15
CHEMBL3797519 — IC50 = 0.7 nM 9.15
CHEMBL3800144 — IC50 = 0.8 nM 9.10
CHEMBL3799695 — IC50 = 0.9 nM 9.05
CHEMBL3797634 — IC50 = 0.9 nM 9.05
CHEMBL3797469 — IC50 = 1.0 nM 9.00
CHEMBL3799326 — IC50 = 1.4 nM 8.85
CHEMBL3800261 — IC50 = 1.4 nM 8.85
CHEMBL3356433 LX-7101 IC50 = 1.6 nM 8.80
CHEMBL3800273 — IC50 = 2.0 nM 8.70
CHEMBL3798406 — IC50 = 3.7 nM 8.43
CHEMBL3800104 — IC50 = 4.5 nM 8.35
CHEMBL3798086 — IC50 = 4.8 nM 8.32
CHEMBL3800515 — IC50 = 7.1 nM 8.15
CHEMBL3798226 — IC50 = 11.0 nM 7.96
CHEMBL3799312 — IC50 = 12.0 nM 7.92
CHEMBL3797875 — IC50 = 12.0 nM 7.92
CHEMBL3797333 — IC50 = 13.0 nM 7.89
CHEMBL3798698 — IC50 = 17.0 nM 7.77
CHEMBL3798729 — IC50 = 22.0 nM 7.66
CHEMBL3797937 — IC50 = 23.0 nM 7.64
CHEMBL3797422 — IC50 = 27.0 nM 7.57
CHEMBL3797769 — IC50 = 31.0 nM 7.51
CHEMBL3799054 — IC50 = 32.0 nM 7.50
CHEMBL3799167 — IC50 = 41.0 nM 7.39
CHEMBL3800555 — IC50 = 62.0 nM 7.21
CHEMBL3800529 — IC50 = 105.0 nM 6.98
CHEMBL3799817 — IC50 = 122.0 nM 6.91
CHEMBL3799060 — IC50 = 700.0 nM 6.16
CHEMBL3798412 — IC50 < 0.1 nM -
CHEMBL3799932 — IC50 < 0.1 nM -
CHEMBL3798651 — IC50 < 0.1 nM -
CHEMBL3798275 — IC50 < 0.1 nM -
CHEMBL3798270 — IC50 < 0.1 nM -
CHEMBL3799358 — IC50 < 0.1 nM -
CHEMBL3798361 — IC50 < 0.1 nM -