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Assay Detail

CHEMBL3391309

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

Binding
Inhibition of LIMK1 (unknown origin) assessed as remaining ATP level using cofilin-2 protein as substrate measured after 60 mins incubation with enzyme by KinaseGlo assay
37
Total Activities
37
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

Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
Sleebs BE, Ganame D, Levit A, Street IP, Gregg A, Falk H, Baell JB
Medchemcomm (2011) 2 : 982 -986
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.41 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3347511 1 7.36
CHEMBL3347507 1 7.30
CHEMBL3347658 1 7.26
CHEMBL3347689 1 6.92
CHEMBL3347682 1 6.90
CHEMBL3347509 1 6.89
CHEMBL3347688 1 6.83
CHEMBL3347681 1 6.81
CHEMBL3347666 1 6.80
CHEMBL3347692 1 6.79
CHEMBL3347510 1 6.76
CHEMBL3347512 1 6.74
CHEMBL3347690 1 6.71
CHEMBL3347679 1 6.70
CHEMBL3347680 1 6.69
CHEMBL3347665 1 6.66
CHEMBL3347677 1 6.64
CHEMBL3347678 1 6.64
CHEMBL3347279 1 6.61
CHEMBL3347657 1 6.58
CHEMBL1836361 1 6.58
CHEMBL3347667 1 6.57
CHEMBL1836360 1 6.52
CHEMBL3347656 1 6.51
CHEMBL3347508 1 6.44
CHEMBL3347691 1 6.42
CHEMBL3347659 1 6.40
CHEMBL3347526 1 6.13
CHEMBL3347660 1 6.10
CHEMBL3347693 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3347511 IC50 = 44.0 nM 7.36
CHEMBL3347507 IC50 = 50.0 nM 7.30
CHEMBL3347658 IC50 = 55.0 nM 7.26
CHEMBL3347689 IC50 = 120.0 nM 6.92
CHEMBL3347682 IC50 = 127.0 nM 6.90
CHEMBL3347509 IC50 = 129.0 nM 6.89
CHEMBL3347688 IC50 = 149.0 nM 6.83
CHEMBL3347681 IC50 = 156.0 nM 6.81
CHEMBL3347666 IC50 = 159.0 nM 6.80
CHEMBL3347692 IC50 = 163.0 nM 6.79
CHEMBL3347510 IC50 = 172.0 nM 6.76
CHEMBL3347512 IC50 = 181.0 nM 6.74
CHEMBL3347690 IC50 = 196.0 nM 6.71
CHEMBL3347679 IC50 = 199.0 nM 6.70
CHEMBL3347680 IC50 = 204.0 nM 6.69
CHEMBL3347665 IC50 = 220.0 nM 6.66
CHEMBL3347677 IC50 = 231.0 nM 6.64
CHEMBL3347678 IC50 = 230.0 nM 6.64
CHEMBL3347279 IC50 = 243.0 nM 6.61
CHEMBL1836361 IC50 = 260.0 nM 6.58
CHEMBL3347657 IC50 = 260.0 nM 6.58
CHEMBL3347667 IC50 = 267.0 nM 6.57
CHEMBL1836360 IC50 = 300.0 nM 6.52
CHEMBL3347656 IC50 = 310.0 nM 6.51
CHEMBL3347508 IC50 = 361.0 nM 6.44
CHEMBL3347691 IC50 = 376.0 nM 6.42
CHEMBL3347659 IC50 = 395.0 nM 6.40
CHEMBL3347526 IC50 = 732.0 nM 6.13
CHEMBL3347660 IC50 = 795.0 nM 6.10
CHEMBL3347693 IC50 = 828.0 nM 6.08
CHEMBL3347663 IC50 = 998.0 nM 6.00
CHEMBL1836359 IC50 = 4000.0 nM 5.40
CHEMBL1836358 IC50 = 7000.0 nM 5.16
CHEMBL457313 IC50 = 9000.0 nM 5.05
CHEMBL211002 IC50 = 33000.0 nM 4.48
CHEMBL207012 IC50 = 37000.0 nM 4.43
CHEMBL3347664 IC50 > 1000.0 nM -