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Assay Detail

CHEMBL5319645

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

Binding
Inhibition of recombinant C-terminal 6His-tagged human BMPR2 (188 to 517 residues) expressed in Escherichia coli Rosetta by LanthaScreen TR-FRET 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-2 (CHEMBL5467)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.
Modukuri RK, Monsivais D, Li F, Palaniappan M, Bohren KM, Tan Z, Ku AF, Wang Y, Madasu C, Li JY, Tang S, Miklossy G, Palmer SS, Young DW, Matzuk MM.
J Med Chem (2023) 66 : 2143 -2160
PubMed 36719862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.76 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5434353 1 5.92
CHEMBL5398151 1 5.80
CHEMBL5404269 1 5.75
CHEMBL5422418 1 5.55
CHEMBL513147 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5434353 IC50 = 1200.0 nM 5.92
CHEMBL5398151 IC50 = 1600.0 nM 5.80
CHEMBL5404269 IC50 = 1800.0 nM 5.75
CHEMBL5422418 IC50 = 2800.0 nM 5.55
CHEMBL513147 IC50 > 1000000.0 nM -