Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL740149

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

Functional
In vitro inhibition of transforming growth factor- beta dependent luciferase growth in mouse fibroblasts (NIH 3T3)
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK, Lampe JW, McCowan JR, McMillen WT, Mort N, Parsons S, Smith EC, Vieth M, Weir LC, Yan L, Zhang F, Yingling JM.
J Med Chem (2003) 46 : 3953 -3956
PubMed 12954047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.48 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341280 1 8.92
CHEMBL129677 1 8.15
CHEMBL118928 1 7.50
CHEMBL125846 1 7.39
CHEMBL129760 1 7.21
CHEMBL340203 1 7.12
CHEMBL261454 1 7.05
CHEMBL129153 1 6.83
CHEMBL125738 1 6.38
CHEMBL129678 1 6.28
CHEMBL338196 1 6.27
CHEMBL126789 1 6.17
CHEMBL126180 1 5.87
CHEMBL338713 1 5.78
CHEMBL129553 1 5.67
CHEMBL337978 1 5.59
CHEMBL130025 1 5.55
CHEMBL126676 1 5.54
CHEMBL341534 1 5.33
CHEMBL129280 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341280 IC50 = 1.2 nM 8.92
CHEMBL129677 IC50 = 7.1 nM 8.15
CHEMBL118928 IC50 = 32.0 nM 7.50
CHEMBL125846 IC50 = 41.0 nM 7.39
CHEMBL129760 IC50 = 61.0 nM 7.21
CHEMBL340203 IC50 = 76.0 nM 7.12
CHEMBL261454 IC50 = 89.0 nM 7.05
CHEMBL129153 IC50 = 148.0 nM 6.83
CHEMBL125738 IC50 = 421.0 nM 6.38
CHEMBL129678 IC50 = 524.0 nM 6.28
CHEMBL338196 IC50 = 538.0 nM 6.27
CHEMBL126789 IC50 = 683.0 nM 6.17
CHEMBL126180 IC50 = 1340.0 nM 5.87
CHEMBL338713 IC50 = 1680.0 nM 5.78
CHEMBL129553 IC50 = 2160.0 nM 5.67
CHEMBL337978 IC50 = 2590.0 nM 5.59
CHEMBL130025 IC50 = 2810.0 nM 5.55
CHEMBL126676 IC50 = 2920.0 nM 5.54
CHEMBL341534 IC50 = 4670.0 nM 5.33
CHEMBL129280 IC50 = 9540.0 nM 5.02