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Assay Detail

CHEMBL5125833

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

Binding
Inhibition of recombinant human N-terminal GST-tagged ALK3 (187 to 532 residues) expressed in baculovirus assessed as loss of peptide phosphorylation activity using peptide substrate in presence of ATP and measured after 1 hrs by HTRF assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bone morphogenetic protein receptor type-1A (CHEMBL5275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Nguyen MH, Atasoylu O, Wu L, Kapilashrami K, Pusey M, Gallagher K, Lai CT, Zhao P, Barbosa J, Liu K, He C, Zhang C, Styduhar ED, Witten MR, Chen Y, Lin L, Yang YO, Covington M, Diamond S, Yeleswaram S, Yao W.
ACS Med Chem Lett (2022) 13 : 1159 -1164
PubMed 35859885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.23 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5184000 1 6.60
CHEMBL5186341 1 6.42
CHEMBL5199417 1 6.27
CHEMBL5181536 1 6.04
CHEMBL5181872 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5184000 IC50 = 251.0 nM 6.60
CHEMBL5186341 IC50 = 383.0 nM 6.42
CHEMBL5199417 IC50 = 538.0 nM 6.27
CHEMBL5181536 IC50 = 901.0 nM 6.04
CHEMBL5181872 IC50 = 1515.0 nM 5.82