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Assay Detail

CHEMBL1036967

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Binding
Inhibition of LIMK1
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

LIM domain kinase 1 (CHEMBL3836)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.
Harrison BA, Whitlock NA, Voronkov MV, Almstead ZY, Gu KJ, Mabon R, Gardyan M, Hamman BD, Allen J, Gopinathan S, McKnight B, Crist M, Zhang Y, Liu Y, Courtney LF, Key B, Zhou J, Patel N, Yates PW, Liu Q, Wilson AG, Kimball SD, Crosson CE, Rice DS, Rawlins DB.
J Med Chem (2009) 52 : 6515 -6518
PubMed 19831390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.60 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570126 1 9.30
CHEMBL570116 1 8.49
CHEMBL565452 1 8.43
CHEMBL570820 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570126 IC50 = 0.5 nM 9.30
CHEMBL570116 IC50 = 3.2 nM 8.49
CHEMBL565452 IC50 = 3.7 nM 8.43
CHEMBL570820 IC50 = 6.6 nM 8.18