Compound name
GSK484
Protein family
Hydrolase
Target name
PADI4
Affinity biochemical (nM)
50
CG-Set
Other targets
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001071aCl
SMILES
COc1cc(C(=O)N2CC[C@@H](O)[C@@H](N)C2)cc2nc(-c3cc4ccccc4n3CC3CC3)n(C)c12.Cl
InChIKey
MULKOGJHUZTANI-ADMBKAPUSA-N
NCBI gene ID
23569
UniProt ID
Q9UM07
Synonyms
PAD, PAD4, PADI5, PDI4, PDI5
Mode of action
Inhibitor
Negative control
GSK106
Affinity biochemical definition
IC50
Affinity biochemical assay type
Fluorescence polarization binding assay (0 mM Ca)
Affinity Biochemical Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4397581/
Affinity biochemical relation
=
Selectivity platform
Panel of kinases, GPCRs, ion channels and transporters (literature)
Selectivity platform number of targets
50
Selectivity remarks
Various assays types used, i.e. TR-FRET, Luminescence assay, FLINT, Electrophysiological assay, LEADseeker SPA; No activation across HDACs 1–11 at 100 μM; Selective for PADI4 over PADI1-3 (tested with recombinant enzymes and cell lysates).
Selectivity Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4397581/