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Assay Detail

CHEMBL5500951

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

Binding
Inhibition of human recombinant GST-tagged ALK5 expressed in baculovirus infected Sf9 insect cells incubated for 60 mins in presence of ATP by microplate scintillation counter
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids.
Meng YQ, Ren J, Sun JX, Guo FY, Min JZ, Nan JX, Quan JS, Lian LH, Jin CH.
Eur J Med Chem (2024) 269 : 116311 -116311
PubMed 38508118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.27 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5558316 1 7.85
CHEMBL5517819 1 7.77
CHEMBL3261090 1 7.66
CHEMBL5517775 1 7.64
CHEMBL5512434 1 7.64
CHEMBL5558398 1 7.60
CHEMBL5556410 1 7.44
CHEMBL5549953 1 7.40
CHEMBL5517800 1 7.21
CHEMBL5557513 1 7.18
CHEMBL5517762 1 7.14
CHEMBL5557604 1 7.08
CHEMBL5558039 1 7.06
CHEMBL5555953 1 7.04
CHEMBL2364611 GALUNISERTIB 2.0 1 6.89
CHEMBL5532435 1 6.50
CHEMBL5517679 1 6.42
CHEMBL5555369 1 -
CHEMBL5558988 1 -
CHEMBL5557444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5558316 IC50 = 14.0 nM 7.85
CHEMBL5517819 IC50 = 17.0 nM 7.77
CHEMBL3261090 IC50 = 22.0 nM 7.66
CHEMBL5517775 IC50 = 23.0 nM 7.64
CHEMBL5512434 IC50 = 23.0 nM 7.64
CHEMBL5558398 IC50 = 25.0 nM 7.60
CHEMBL5556410 IC50 = 36.0 nM 7.44
CHEMBL5549953 IC50 = 40.0 nM 7.40
CHEMBL5517800 IC50 = 61.0 nM 7.21
CHEMBL5557513 IC50 = 66.0 nM 7.18
CHEMBL5517762 IC50 = 73.0 nM 7.14
CHEMBL5557604 IC50 = 84.0 nM 7.08
CHEMBL5558039 IC50 = 87.0 nM 7.06
CHEMBL5555953 IC50 = 92.0 nM 7.04
CHEMBL2364611 GALUNISERTIB IC50 = 129.0 nM 6.89
CHEMBL5532435 IC50 = 317.0 nM 6.50
CHEMBL5517679 IC50 = 377.0 nM 6.42
CHEMBL5555369 IC50 - -
CHEMBL5558988 IC50 - -
CHEMBL5557444 IC50 - -