GNE-2256

Inhibitor of IRAK4

Structure

SERP Rating

Probe GNE-2256 is in the process of SERP review.

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Information

IRAK4

Inhibitor

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: Q9NWZ3

Target Class: Kinase

Target SubClass: TKL

Potency: Ki

Potency Value: 1.4 ±0.32 nM

Potency Assay: Biochemical Assay (FRET)

PDB ID for probe-target interaction (3D structure): 6UYA

Target aliases:

Interleukin-1 receptor-associated kinase 4, IRAK4, ...

DOI Reference: 10.1021/acsmedchemlett.9b00380

Uniprot ID: Q9NWZ3

Target Class: Kinase

Target SubClass: TKL

Potency: Inhibition

Potency Value: 80 ± 9.2 %

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): 6UYA

Target aliases:

Interleukin-1 receptor-associated kinase 4, IRAK4, ...

DOI Reference: 10.1021/acsmedchemlett.9b00380

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - Kinase panel (221) at 1 µM: Closest off-targets (IC50 [nM]) are FLT3 (177), JAK1 (282), JAK2 (486), LRRK2 (198), MAP4K4 (680), MINK1 (879), MAP3K7- TAB1 (TAK1-TAB1) (966), NTRK1 (313), NTRK2 (259). Selectivity outside target family - CEREP panel (36) at 1 µM: Off-targets with > 50% inhibition are TACR1 (NK1), HTR2B, ACHE.

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SERP ratings and comments

No SERP comments found for GNE-2256