FIDRISERTIB

FIDRISERTIB : Inhibitor of ACVR1

Structure

SERP Rating

Probe FIDRISERTIB is in the process of SERP review.

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Information

ACVR1 (Mutant:WT, R206H)

Inhibitor

up to 100 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q04771

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 0.2 nM

Potency Assay: LanthaScreen binding assays using ALK2-R206H

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

Target aliases:

Activin receptor type-1, ACVRLK2, ACVR1, ACVR1_HUM ...

DOI Reference: 10.1126/scitranslmed.abp8334

Uniprot ID: Q04771

Target Class: Kinase

Target SubClass: TKL

Potency: IC50

Potency Value: 0.6 nM

Potency Assay: LanthaScreen binding assays using WT-ALK2

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

Target aliases:

Activin receptor type-1, ACVRLK2, ACVR1, ACVR1_HUM ...

DOI Reference: 10.1126/scitranslmed.abp8334

Uniprot ID: Q04771

Target Class: Kinase

Target SubClass: TKL

Potency: Kd

Potency Value: 1.2 nM

Potency Assay: Biochemical assay using recombinant ALK2-R206H

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

Target aliases:

Activin receptor type-1, ACVRLK2, ACVR1, ACVR1_HUM ...

DOI Reference: 10.1126/scitranslmed.abp8334

Uniprot ID: Q04771

Target Class: Kinase

Target SubClass: TKL

Potency: Kd

Potency Value: 2.1 nM

Potency Assay: Biochemical assay using recombinant ALK2-WT

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

Target aliases:

Activin receptor type-1, ACVRLK2, ACVR1, ACVR1_HUM ...

DOI Reference: 10.1126/scitranslmed.abp8334

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Kinome profiling of BLU-782 showed high selectivity, with only four kinases exhibiting <100 nM protein binding affinity (WT, R206H, ALK-4, -6). In biochemical binding assays, BLU-782 potently bound ALK2-R206H, with at least 15-fold selectivity over other BMP type I and type II ALK family receptors.

Potency assay, off target (cells): Cellular IC50 values showed >100-fold selectivity of BLU-782 for ALK2-R206H over ALK1, ALK3, and ALK6.

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