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Assay Detail

CHEMBL3411298

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Binding
Inhibition of human Limk1 using cofilin substrate, ATP and [gamma33P]ATP
ChEMBL ↗
45
Total Activities
45
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

Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.
Yin Y, Zheng K, Eid N, Howard S, Jeong JH, Yi F, Guo J, Park CM, Bibian M, Wu W, Hernandez P, Park H, Wu Y, Luo JL, LoGrasso PV, Feng Y.
J Med Chem (2015) 58 : 1846 -1861
PubMed 25621531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.97 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3410056 — — 1 8.10
CHEMBL3407526 — — 1 7.75
CHEMBL3410055 — — 1 7.72
CHEMBL3410052 — — 1 7.70
CHEMBL3410054 — — 1 7.68
CHEMBL3410053 — — 1 7.68
CHEMBL3410050 — — 1 7.68
CHEMBL3410042 — — 1 7.60
CHEMBL3410049 — — 1 7.57
CHEMBL3410032 — — 1 7.46
CHEMBL3410045 — — 1 7.43
CHEMBL3410036 — — 1 7.37
CHEMBL3410051 — — 1 7.33
CHEMBL3410048 — — 1 7.28
CHEMBL3410040 — — 1 7.24
CHEMBL3410026 — — 1 7.22
CHEMBL1951346 — — 1 7.21
CHEMBL3410041 — — 1 7.17
CHEMBL3410031 — — 1 7.12
CHEMBL3410025 — — 1 7.10
CHEMBL3410024 — — 1 7.10
CHEMBL3410039 — — 1 7.07
CHEMBL3410038 — — 1 7.00
CHEMBL3410047 — — 1 7.00
CHEMBL3410037 — — 1 6.88
CHEMBL3410028 — — 1 6.85
CHEMBL3410044 — — 1 6.82
CHEMBL1951344 — — 1 6.70
CHEMBL3410033 — — 1 6.69
CHEMBL3410030 — — 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3410056 — IC50 = 8.0 nM 8.10
CHEMBL3407526 — IC50 = 18.0 nM 7.75
CHEMBL3410055 — IC50 = 19.0 nM 7.72
CHEMBL3410052 — IC50 = 20.0 nM 7.70
CHEMBL3410054 — IC50 = 21.0 nM 7.68
CHEMBL3410053 — IC50 = 21.0 nM 7.68
CHEMBL3410050 — IC50 = 21.0 nM 7.68
CHEMBL3410042 — IC50 = 25.0 nM 7.60
CHEMBL3410049 — IC50 = 27.0 nM 7.57
CHEMBL3410032 — IC50 = 35.0 nM 7.46
CHEMBL3410045 — IC50 = 37.0 nM 7.43
CHEMBL3410036 — IC50 = 43.0 nM 7.37
CHEMBL3410051 — IC50 = 47.0 nM 7.33
CHEMBL3410048 — IC50 = 53.0 nM 7.28
CHEMBL3410040 — IC50 = 58.0 nM 7.24
CHEMBL3410026 — IC50 = 60.0 nM 7.22
CHEMBL1951346 — IC50 = 62.0 nM 7.21
CHEMBL3410041 — IC50 = 67.0 nM 7.17
CHEMBL3410031 — IC50 = 75.0 nM 7.12
CHEMBL3410025 — IC50 = 80.0 nM 7.10
CHEMBL3410024 — IC50 = 80.0 nM 7.10
CHEMBL3410039 — IC50 = 86.0 nM 7.07
CHEMBL3410038 — IC50 = 101.0 nM 7.00
CHEMBL3410047 — IC50 = 100.0 nM 7.00
CHEMBL3410037 — IC50 = 132.0 nM 6.88
CHEMBL3410028 — IC50 = 142.0 nM 6.85
CHEMBL3410044 — IC50 = 151.0 nM 6.82
CHEMBL1951344 — IC50 = 201.0 nM 6.70
CHEMBL3410033 — IC50 = 203.0 nM 6.69
CHEMBL3410030 — IC50 = 283.0 nM 6.55
CHEMBL3410029 — IC50 = 315.0 nM 6.50
CHEMBL3410043 — IC50 = 350.0 nM 6.46
CHEMBL3410035 — IC50 = 368.0 nM 6.43
CHEMBL3410027 — IC50 = 710.0 nM 6.15
CHEMBL3410046 — IC50 = 913.0 nM 6.04
CHEMBL3410057 — IC50 = 1090.0 nM 5.96
CHEMBL3410023 — IC50 = 1527.0 nM 5.82
CHEMBL3410034 — IC50 = 4507.0 nM 5.35
CHEMBL3410058 — IC50 = 9240.0 nM 5.03
CHEMBL3410022 — IC50 > 10000.0 nM -
CHEMBL1951443 — IC50 > 10000.0 nM -
CHEMBL1951441 — IC50 > 10000.0 nM -
CHEMBL1951349 — IC50 > 10000.0 nM -
CHEMBL1951350 — IC50 > 10000.0 nM -
CHEMBL3410059 — IC50 > 10000.0 nM -