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Assay Detail

CHEMBL4263991

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of BMP6-induced ALK2 transcriptional activity in mouse C2C12 cells expressing BRE-Luc after 30 mins by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type C2C12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Activin receptor type-1 (CHEMBL3309042)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors.
Jiang JK, Huang X, Shamim K, Patel PR, Lee A, Wang AQ, Nguyen K, Tawa G, Cuny GD, Yu PB, Zheng W, Xu X, Sanderson P, Huang W.
Bioorg Med Chem Lett (2018) 28 : 3356 -3362
PubMed 30227946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.66 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4283638 1 8.10
CHEMBL513147 1 7.85
CHEMBL4288921 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4283638 EC50 = 8.0 nM 8.10
CHEMBL513147 EC50 = 14.0 nM 7.85
CHEMBL4288921 EC50 = 91.0 nM 7.04