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Assay Detail

CHEMBL747420

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

Binding
Tested for inhibition of Myosin light chain kinase from chicken gizzard
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Meleagris gallopavo
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Myosin light chain kinase, smooth muscle (CHEMBL2428)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel indolocarbazole protein kinase c inhibitors with improved biochemical and physicochemical properties
Kleinschroth J, Hartenstein J, Rudolph C, Schachtele C
Bioorg Med Chem Lett (1995) 5 : 55 -60
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.68 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 8.00
CHEMBL155929 1 7.75
CHEMBL348563 1 7.52
CHEMBL156433 1 7.50
CHEMBL347154 1 7.31
CHEMBL348177 1 7.26
CHEMBL156172 1 6.92
CHEMBL157822 1 6.92
CHEMBL348902 1 6.75
CHEMBL345593 1 6.70
CHEMBL157967 1 6.66
CHEMBL157892 1 6.60
CHEMBL157528 1 6.51
CHEMBL154245 1 6.41
CHEMBL346467 1 5.80
CHEMBL346038 1 5.26
CHEMBL302449 GO-6976 1 5.24
CHEMBL345639 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 10.0 nM 8.00
CHEMBL155929 IC50 = 18.0 nM 7.75
CHEMBL348563 IC50 = 30.0 nM 7.52
CHEMBL156433 IC50 = 32.0 nM 7.50
CHEMBL347154 IC50 = 49.0 nM 7.31
CHEMBL348177 IC50 = 55.0 nM 7.26
CHEMBL156172 IC50 = 120.0 nM 6.92
CHEMBL157822 IC50 = 120.0 nM 6.92
CHEMBL348902 IC50 = 180.0 nM 6.75
CHEMBL345593 IC50 = 200.0 nM 6.70
CHEMBL157967 IC50 = 220.0 nM 6.66
CHEMBL157892 IC50 = 250.0 nM 6.60
CHEMBL157528 IC50 = 310.0 nM 6.51
CHEMBL154245 IC50 = 390.0 nM 6.41
CHEMBL346467 IC50 = 1600.0 nM 5.80
CHEMBL346038 IC50 = 5500.0 nM 5.26
CHEMBL302449 GO-6976 IC50 = 5800.0 nM 5.24
CHEMBL345639 IC50 = 9200.0 nM 5.04