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Assay Detail

CHEMBL4178569

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

Binding
Binding affinity to human PAD2 expressed in HEK293T cells assessed as decrease in histone H3 citrulination incubated for 3 hrs in presence of ionomycin/CaCl2 by SDS-PAGE analysis
5
Total Activities
5
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

Protein-arginine deiminase type-2 (CHEMBL1909487)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Selective Inhibitor of Protein Arginine Deiminase 2.
Muth A, Subramanian V, Beaumont E, Nagar M, Kerry P, McEwan P, Srinath H, Clancy K, Parelkar S, Thompson PR.
J Med Chem (2017) 60 : 3198 -3211
PubMed 28328217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.84 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4214962 1 6.40
CHEMBL4204476 1 5.92
CHEMBL4202689 1 5.68
CHEMBL4217485 1 5.62
CHEMBL4211403 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4214962 EC50 = 400.0 nM 6.40
CHEMBL4204476 EC50 = 1200.0 nM 5.92
CHEMBL4202689 EC50 = 2100.0 nM 5.68
CHEMBL4217485 EC50 = 2400.0 nM 5.62
CHEMBL4211403 EC50 = 2700.0 nM 5.57