SGC-AAK1-1

SGC-AAK1-1 : Inhibitor of AAK1 and BMP2K

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 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 SGC-AAK1-1 is in the process of SERP review.

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Information

AAK1
BMP2K

Inhibitor

up to 5 uM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q2M2I8

Target Class: Kinase

Target SubClass: Ser/Thr kinase

Potency: Ki

Potency Value: 9.1 nM

Potency Assay: TR-FRET binding assays

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

Target aliases:

AP2-associated protein kinase 1, KIAA1048, AAK1, A ...

DOI Reference: 10.1021/acsmedchemlett.9b00399

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Tested in KINOMEscan (DiscoverX) against 403 wildtype human protein kinases at 1 μM, it proved to be highly selective with only 3 kinase off-targets: RIOK1 (KD = 72), RIOK3 (KD = 290), and PIP5K1C (KD = 260).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

SGC-AAK1-1 is a clean in vitro tool compound with decent biochemical potency, weak but selective cellular active. The upside of this compound is its kinome selectivity. The downside is its relatively modest cellular potency and lack of in vivo exposure. Investigators interested in AAK1 should also consider using BMT-090605, LP-935509, or BMS-986176/LX-9211, which are 3 literature compounds from different scaffolds and all commercially available (e.g., MedChemExpress). BMS-986176/LX-9211 in particular has reported kinome selectivity, exquisite potency, and good in vivo exposure. As a side note, LX9211 has been reported to show positive benefits in clinical trial for diabetic neuropathic pain. Combined use of multiple probes is recommended to avoid off-target effects.

(last updated: 8 Feb 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

Cell potency for AAK1 is less than 1 μM, but for BMP2K is 2.8 μM thus, it could be improved. Additional assays could be performed to gain more information regarding effect on endogenous protein. No cytotoxicity data were mentioned.

(last updated: 23 May 2024 )