APAFANT

APAFANT : Antagonist of PTAFR

Structure

SERP Rating

In Cells

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In Model Organisms

(1 ratings)

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Probe APAFANT is in the process of SERP review.

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Information

PTAFR

Antagonist

use at 300 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P25105

Target Class: GPCR

Target SubClass: Platelet-activating factor receptor

Potency: Ki

Potency Value: 9.9 nM

Potency Assay: Competition with [3H]PAF binding to human platelets

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

Target aliases:

Platelet-activating factor receptor, PAFR, PTAFR, ...

PMID Reference: 3598913

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Eurofins Safety screen (44 targets) at 10 µM [% Ctrl]: BZD/CENTR (rat) (12), PTGS2 (47); Benzodiazepine receptor inhibition (rat): Ki = 388 nM.

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SERP ratings and comments

SERP Ratings

In Model Organisms

SERP Comments:

The paper currently being cited for "In Vivo Validations" (i.e., PMID 3598913) highlights the following regarding the dosing of rats: "In anesthetized rats, the hypotension induced by an i.v. PAF infusion was also reversed [by WEB 2086] (ED50 = 0.052 mg/kg i.v.)." This i.v. dosing is not congruent with the specified Delivery Method of "Oral" nor the Dose of "11 microMolar/kg".

(last updated: 11 Jul 2024 )