PF-06648671

PF-06648671 : Modulator of PSEN1

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe PF-06648671 is in the process of SERP review.

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Information

PSEN1

Modulator

up to 1 uM

Probe Availability:

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Good selectivity was achieved over Notch (Notch intracellular domain, NICD) and hERG (>1,600-fold and >1,020-fold, respectively)

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a well-characterised chemical probe. The data supporting potency, cellular efficacy and in vivo efficacy are well-described and use accepted models. The main limitation with regards to use of this probe is a paucity of selectivity data. In rat, 40 mg/kg gives greater efficacy than 10 mg/kg. In the dog I'd recommend the 20 mg/kg dose which has clear efficacy

(last updated: 12 Dec 2024 )