PAD-PF2

PAD-PF2 : allosteric inhibitor of PADI1, PADI2, PADI3 and PADI4

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe PAD-PF2 is in the process of SERP review.

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Information

PADI1
PADI2
PADI3
PADI4

allosteric

up to 10 uM

In Vitro Validations

Uniprot ID: Q9ULC6

Target Class: Enzyme

Target SubClass: Deiminase

Potency: IC50

Potency Value: 109 nM

Potency Assay: Glutamate dehydrogenase (GDH) enzyme-coupled assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Protein-arginine deiminase type-1, PDI1, PAD1, PAD ...

DOI Reference: 10.1038/s41467-025-59919-4

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): The target specificity of PAD-PF2 was evaluated by profiling the compound against a diverse panel of receptors, enzymes, kinases, transporters, and ion channels at a dose of 10 µM concentration . PAD-PF2 showed > 80-fold selectivity relative to the PAD4 enzymatic IC50 value. Among the targets tested above, PAD-PF2 was found to be a weak agonist of the κ-opioid receptor (EC50 = 7.55 µM, 177-fold) and weak antagonist of the M1 muscarinic acetylcholine receptor (IC50 = 12.3 µM, 288-fold). Also, weak binding affinity was observed to the choline transporter (Ki = 3.45 µM, 81-fold) and the L-type calcium ion channel (Ki = 11.1 µM, 260-fold).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Overall, this probe seems to be clearly investigated and the data in the paper (DOI: 10.1038/s41467-025-59919-4) is in-depth. This probe is definitely useful as a PAD probe, but may be useful in combination with active site PAD probes.

(last updated: 27 May 2025 )