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Assay Detail

CHEMBL4034243

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

Binding
Induction of nuclear translocation of human GFP-tagged NFATc1 expressed in virus infected primary human skeletal muscle myoblasts after 3 hrs by DAPI staining based assay
33
Total Activities
33
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

Nuclear factor of activated T-cells, cytoplasmic 1 (CHEMBL3876)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.
Shaw SJ, Goff DA, Lin N, Singh R, Li W, McLaughlin J, Baltgalvis KA, Payan DG, Kinsella TM.
Bioorg Med Chem Lett (2017) 27 : 2617 -2621
PubMed 28408219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 5.26 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4064316 1 6.51
CHEMBL4105629 1 5.80
CHEMBL4077010 1 5.66
CHEMBL4084955 1 5.53
CHEMBL4079572 1 5.32
CHEMBL4098505 1 5.31
CHEMBL4075648 1 5.28
CHEMBL4095674 1 5.16
CHEMBL4091320 1 5.16
CHEMBL4069163 1 5.12
CHEMBL4090889 1 5.01
CHEMBL4080488 1 4.68
CHEMBL4072138 1 4.66
CHEMBL4066607 1 4.37
CHEMBL4098364 1 -
CHEMBL4066075 1 -
CHEMBL4095156 1 -
CHEMBL1802401 1 -
CHEMBL1802963 1 -
CHEMBL4087456 1 -
CHEMBL4065388 1 -
CHEMBL3421979 1 -
CHEMBL4074685 1 -
CHEMBL4103831 1 -
CHEMBL4095479 1 -
CHEMBL4073997 1 -
CHEMBL269538 HARMINE 1.0 1 -
CHEMBL4094549 1 -
CHEMBL4068096 1 -
CHEMBL4069088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4064316 EC50 = 310.0 nM 6.51
CHEMBL4105629 EC50 = 1590.0 nM 5.80
CHEMBL4077010 EC50 = 2210.0 nM 5.66
CHEMBL4084955 EC50 = 2980.0 nM 5.53
CHEMBL4079572 EC50 = 4800.0 nM 5.32
CHEMBL4098505 EC50 = 4850.0 nM 5.31
CHEMBL4075648 EC50 = 5310.0 nM 5.28
CHEMBL4095674 EC50 = 6960.0 nM 5.16
CHEMBL4091320 EC50 = 6900.0 nM 5.16
CHEMBL4069163 EC50 = 7580.0 nM 5.12
CHEMBL4090889 EC50 = 9800.0 nM 5.01
CHEMBL4080488 EC50 = 20820.0 nM 4.68
CHEMBL4072138 EC50 = 21700.0 nM 4.66
CHEMBL4066607 EC50 = 42980.0 nM 4.37
CHEMBL48082 EC50 - -
CHEMBL4102903 EC50 - -
CHEMBL4086818 EC50 - -
CHEMBL4098364 EC50 - -
CHEMBL4066075 EC50 - -
CHEMBL4095156 EC50 - -
CHEMBL1802401 EC50 - -
CHEMBL1802963 EC50 - -
CHEMBL4087456 EC50 - -
CHEMBL4065388 EC50 - -
CHEMBL3421979 EC50 - -
CHEMBL4074685 EC50 - -
CHEMBL4103831 EC50 - -
CHEMBL4095479 EC50 - -
CHEMBL4073997 EC50 - -
CHEMBL269538 HARMINE EC50 - -
CHEMBL4094549 EC50 - -
CHEMBL4068096 EC50 - -
CHEMBL4069088 EC50 - -