FIDRISERTIB

FIDRISERTIB : Inhibitor of ACVR1

Structure

SERP Rating

In Cells

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In Model Organisms

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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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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Selectivity of Fidrisertib (Blu-782, IPN60130) has been determined by KinomeScan and in cells using constitutively active ALK1-6 receptor kinases, but data is lacking for BMP vs activin vs TGF-beta ligand-induced signaling in cells. Since ALK4 displays an in vitro IC50 value of 65 nM, cellular readouts using 100 nM compound will not be as clean as other potential chemical probes for this family.

(last updated: 17 Feb 2026 )