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Assay Detail

CHEMBL745132

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

Binding
Inhibitory activity against MLCK (smooth muscle myosin light chain kinase)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Myosin light chain kinase, smooth muscle (CHEMBL3062)
Type SINGLE PROTEIN
Organism Gallus gallus

Publication

Identification of novel classes of protein kinase inhibitors using combinatorial peptide chemistry based on functional genomics knowledge.
Lukas TJ, Mirzoeva S, Slomczynska U, Watterson DM.
J Med Chem (1999) 42 : 910 -919
PubMed 10072688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.42 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL385812 1 7.40
CHEMBL443574 1 7.30
CHEMBL268790 1 6.96
CHEMBL425624 1 6.92
CHEMBL409544 1 6.82
CHEMBL267348 1 6.82
CHEMBL265891 1 6.80
CHEMBL262895 1 6.80
CHEMBL404932 1 6.70
CHEMBL216528 1 6.66
CHEMBL415435 1 6.57
CHEMBL262286 1 6.54
CHEMBL265875 1 6.54
CHEMBL264533 1 6.52
CHEMBL262494 1 6.51
CHEMBL386668 1 6.50
CHEMBL412772 1 6.44
CHEMBL264293 1 6.38
CHEMBL405953 1 6.21
CHEMBL1791266 1 6.14
CHEMBL269727 1 6.06
CHEMBL411670 1 5.98
CHEMBL264267 1 5.53
CHEMBL407521 1 4.70
CHEMBL430273 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL385812 IC50 = 40.0 nM 7.40
CHEMBL443574 IC50 = 50.0 nM 7.30
CHEMBL268790 IC50 = 110.0 nM 6.96
CHEMBL425624 IC50 = 120.0 nM 6.92
CHEMBL409544 IC50 = 150.0 nM 6.82
CHEMBL267348 IC50 = 150.0 nM 6.82
CHEMBL265891 IC50 = 160.0 nM 6.80
CHEMBL262895 IC50 = 160.0 nM 6.80
CHEMBL404932 IC50 = 200.0 nM 6.70
CHEMBL216528 IC50 = 220.0 nM 6.66
CHEMBL415435 IC50 = 270.0 nM 6.57
CHEMBL262286 IC50 = 290.0 nM 6.54
CHEMBL265875 IC50 = 290.0 nM 6.54
CHEMBL264533 IC50 = 300.0 nM 6.52
CHEMBL262494 IC50 = 310.0 nM 6.51
CHEMBL386668 IC50 = 320.0 nM 6.50
CHEMBL412772 IC50 = 360.0 nM 6.44
CHEMBL264293 IC50 = 420.0 nM 6.38
CHEMBL405953 IC50 = 610.0 nM 6.21
CHEMBL1791266 IC50 = 730.0 nM 6.14
CHEMBL269727 IC50 = 870.0 nM 6.06
CHEMBL411670 IC50 = 1040.0 nM 5.98
CHEMBL264267 IC50 = 2970.0 nM 5.53
CHEMBL407521 IC50 = 20000.0 nM 4.70
CHEMBL430273 IC50 = 20000.0 nM 4.70