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Assay Detail

CHEMBL3365509

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

Binding
Inhibition of purified human ALK5 kinase after 45 mins by liquid scintillation counting in presence of ATP [gamma-32P]
25
Total Activities
25
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

TGF-beta receptor type-1 (CHEMBL4439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Mohedas AH, Wang Y, Sanvitale CE, Canning P, Choi S, Xing X, Bullock AN, Cuny GD, Yu PB.
J Med Chem (2014) 57 : 7900 -7915
PubMed 25101911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.77 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3341794 1 7.52
CHEMBL3341944 1 7.31
CHEMBL3341943 1 6.75
CHEMBL3341945 1 6.73
CHEMBL3341787 1 6.62
CHEMBL1230714 1 6.55
CHEMBL3341947 1 6.00
CHEMBL3341951 1 5.85
CHEMBL3341952 1 5.72
CHEMBL3341789 1 5.52
CHEMBL3341792 1 5.30
CHEMBL3341946 1 5.16
CHEMBL3341948 1 4.91
CHEMBL3341949 1 4.82
CHEMBL3341953 1 4.68
CHEMBL3341791 1 4.68
CHEMBL3341793 1 4.00
CHEMBL3341790 1 -
CHEMBL3341795 1 -
CHEMBL3341788 1 -
CHEMBL3341955 1 -
CHEMBL3341954 1 -
CHEMBL3341950 1 -
CHEMBL3341942 1 -
CHEMBL3341941 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3341794 IC50 = 30.0 nM 7.52
CHEMBL3341944 IC50 = 49.0 nM 7.31
CHEMBL3341943 IC50 = 180.0 nM 6.75
CHEMBL3341945 IC50 = 186.0 nM 6.73
CHEMBL3341787 IC50 = 240.0 nM 6.62
CHEMBL1230714 IC50 = 280.0 nM 6.55
CHEMBL3341947 IC50 = 1000.0 nM 6.00
CHEMBL3341951 IC50 = 1400.0 nM 5.85
CHEMBL3341952 IC50 = 1910.0 nM 5.72
CHEMBL3341789 IC50 = 3000.0 nM 5.52
CHEMBL3341792 IC50 = 5000.0 nM 5.30
CHEMBL3341946 IC50 = 6900.0 nM 5.16
CHEMBL3341948 IC50 = 12300.0 nM 4.91
CHEMBL3341949 IC50 = 15000.0 nM 4.82
CHEMBL3341953 IC50 = 21000.0 nM 4.68
CHEMBL3341791 IC50 = 21000.0 nM 4.68
CHEMBL3341793 IC50 = 99000.0 nM 4.00
CHEMBL3341790 IC50 - -
CHEMBL3341795 IC50 - -
CHEMBL3341788 IC50 - -
CHEMBL3341955 IC50 - -
CHEMBL3341954 IC50 - -
CHEMBL3341950 IC50 - -
CHEMBL3341942 IC50 - -
CHEMBL3341941 IC50 - -