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Assay Detail

CHEMBL3227038

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

Binding
Inhibition of LIMK1 (unknown origin) using cofilin-2 as substrate after 60 mins by Kinase-Glo assay
41
Total Activities
41
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

Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
Sleebs BE, Levit A, Street IP, Falk H, Hammonds T, Wong AC, Charles MD, Olson MF, Baell JB
Medchemcomm (2011) 2 : 977 -981
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.08 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1836361 1 6.58
CHEMBL1836360 1 6.52
CHEMBL3219028 1 6.16
CHEMBL3219008 1 5.89
CHEMBL3219011 1 5.80
CHEMBL3219012 1 5.70
CHEMBL1483395 1 5.55
CHEMBL1571017 1 5.52
CHEMBL3219024 1 5.40
CHEMBL1836359 1 5.40
CHEMBL3219025 1 5.26
CHEMBL3219026 1 5.24
CHEMBL3219027 1 5.21
CHEMBL1836358 1 5.16
CHEMBL1269082 1 5.15
CHEMBL377085 1 5.05
CHEMBL457313 1 5.05
CHEMBL3218815 1 4.96
CHEMBL3219023 1 4.82
CHEMBL3219009 1 4.52
CHEMBL211002 1 4.48
CHEMBL3219018 1 4.47
CHEMBL207012 1 4.43
CHEMBL578181 1 4.43
CHEMBL3219010 1 4.39
CHEMBL3219029 1 4.37
CHEMBL2153531 1 4.37
CHEMBL3219013 1 4.36
CHEMBL568904 1 4.25
CHEMBL3219021 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1836361 IC50 = 260.0 nM 6.58
CHEMBL1836360 IC50 = 300.0 nM 6.52
CHEMBL3219028 IC50 = 700.0 nM 6.16
CHEMBL3219008 IC50 = 1300.0 nM 5.89
CHEMBL3219011 IC50 = 1600.0 nM 5.80
CHEMBL3219012 IC50 = 2000.0 nM 5.70
CHEMBL1483395 IC50 = 2800.0 nM 5.55
CHEMBL1571017 IC50 = 3000.0 nM 5.52
CHEMBL3219024 IC50 = 4000.0 nM 5.40
CHEMBL1836359 IC50 = 4000.0 nM 5.40
CHEMBL3219025 IC50 = 5500.0 nM 5.26
CHEMBL3219026 IC50 = 5700.0 nM 5.24
CHEMBL3219027 IC50 = 6100.0 nM 5.21
CHEMBL1836358 IC50 = 7000.0 nM 5.16
CHEMBL1269082 IC50 = 7100.0 nM 5.15
CHEMBL377085 IC50 = 9000.0 nM 5.05
CHEMBL457313 IC50 = 9000.0 nM 5.05
CHEMBL3218815 IC50 = 11000.0 nM 4.96
CHEMBL3219023 IC50 = 15000.0 nM 4.82
CHEMBL3219009 IC50 = 30000.0 nM 4.52
CHEMBL211002 IC50 = 33000.0 nM 4.48
CHEMBL3219018 IC50 = 34000.0 nM 4.47
CHEMBL207012 IC50 = 37000.0 nM 4.43
CHEMBL578181 IC50 = 37000.0 nM 4.43
CHEMBL3219010 IC50 = 41000.0 nM 4.39
CHEMBL3219029 IC50 = 43000.0 nM 4.37
CHEMBL2153531 IC50 = 43000.0 nM 4.37
CHEMBL3219013 IC50 = 44000.0 nM 4.36
CHEMBL568904 IC50 = 56000.0 nM 4.25
CHEMBL3219021 IC50 = 92000.0 nM 4.04
CHEMBL3219014 IC50 > 100000.0 nM -
CHEMBL3217769 IC50 > 100000.0 nM -
CHEMBL3219015 IC50 > 100000.0 nM -
CHEMBL3219016 IC50 > 100000.0 nM -
CHEMBL3219017 IC50 > 100000.0 nM -
CHEMBL3219019 IC50 > 100000.0 nM -
CHEMBL538197 IC50 > 100000.0 nM -
CHEMBL3219020 IC50 > 100000.0 nM -
CHEMBL3219022 IC50 > 100000.0 nM -
CHEMBL2153541 IC50 > 100000.0 nM -
CHEMBL3219030 IC50 > 50000.0 nM -