Biological Information

Background Information:

The NanoBRET™ Target Engagement (TE) Intracellular Kinase Assays are based on the Bioluminescence Resonance Energy Transfer (BRET) system, an energy transfer technique designed to measure molecular proximity in living cells. The assay measures the apparent affinity of test compounds by competitive displacement of the NanoBRET™ tracer, reversibly bound to a NanoLuc® luciferase-kinase fusion expressed in cells.

Family:

Kinase

Sub Family:

RSTK

Class:

Protein Ser/Thr

Protein Name:

ALK2

Uniprot Number:

Q04771

Protein Aliases:

Activin receptor type I|ACTR-I|Activin receptor-like kinase 2|ALK-2|Serine/threonine-protein kinase receptor R1|SKR1|TGF-B superfamily receptor type I|TSR-I

Gene Name:

ACVR1

Gene ID:

90

Gene Aliases:

FOP| ALK2| SKR1| TSRI| ACTRI| ACVR1A| ACVRLK2

Accession Number:

NM_001111067

Organism:

Human

Construct Details:

NanoLuc® luciferase fused to the C-terminus of the Wild Type Full-length kinase

Cell Type:

293H

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based Binding

Functional Mode:

Antagonist

Detection Method:

NanoBRET

Testing Information

Procedure Summary:

NanoBRET TE Intracellular Kinase Assays are performed according to Promega Adherent Format Assay Protocol using NanoBRET™ Tracer K-11. 293H cells are transfected with ACVR1-NanoLuc® Fusion Vector, seeded in 384-well plates, and cultivated overnight. Target engagement of compounds are measured by treating the cells with the compound in presence of a fixed concentration of fluorescent tracer.

Tracer:

K-11 (0.068 µM)

Incubation:

120 min at 37°C

Test Sample Requirements:

Minimum 1) Dose Response: 120 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 30 µM)

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

16038120

Name

TAE-684

Measurement

7140nM - IC50

PubChem ID

45111335

Name

APY-69

Measurement

70nM - IC50

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault