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Assay Detail

CHEMBL4739183

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

Binding
Inhibition of recombinant human GST-fused ALK5 expressed in baculovirus infected Sf9 cells assessed as incoporation of [33]Pi after 60 mins in presence of [gamma-33P]-ATP by microplate scintillation counter method
16
Total Activities
16
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 evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38α MAP inhibitors.
Liu YY,Guo Z,Wang JY,Wang HM,Da Qi J,Ma J,Piao HR,Jin CH,Jin X
Eur J Med Chem (2021) 216 : 113311 -113311
PubMed 33677350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.94 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4748823 1 8.40
CHEMBL4778963 1 8.40
CHEMBL4779584 1 8.30
CHEMBL4747557 1 8.30
CHEMBL4780141 1 8.22
CHEMBL4759911 1 8.10
CHEMBL4798879 1 8.05
CHEMBL4788508 1 8.00
CHEMBL4794179 1 7.96
CHEMBL4752915 1 7.89
CHEMBL4756404 1 7.85
CHEMBL3260567 VACTOSERTIB 2.0 1 7.85
CHEMBL4784124 1 7.80
CHEMBL4780013 1 7.62
CHEMBL4740767 1 7.47
CHEMBL2364611 GALUNISERTIB 2.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4748823 IC50 = 4.0 nM 8.40
CHEMBL4778963 IC50 = 4.0 nM 8.40
CHEMBL4779584 IC50 = 5.0 nM 8.30
CHEMBL4747557 IC50 = 5.0 nM 8.30
CHEMBL4780141 IC50 = 6.0 nM 8.22
CHEMBL4759911 IC50 = 8.0 nM 8.10
CHEMBL4798879 IC50 = 9.0 nM 8.05
CHEMBL4788508 IC50 = 10.0 nM 8.00
CHEMBL4794179 IC50 = 11.0 nM 7.96
CHEMBL4752915 IC50 = 13.0 nM 7.89
CHEMBL4756404 IC50 = 14.0 nM 7.85
CHEMBL3260567 VACTOSERTIB IC50 = 14.0 nM 7.85
CHEMBL4784124 IC50 = 16.0 nM 7.80
CHEMBL4780013 IC50 = 24.0 nM 7.62
CHEMBL4740767 IC50 = 34.0 nM 7.47
CHEMBL2364611 GALUNISERTIB IC50 = 129.0 nM 6.89