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Assay Detail

CHEMBL861568

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

Functional
Inhibitory activity against TGF-beta-stimulated proliferation in NIH3T3 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD, Wagner JR, Britt K, Lu KX, McMillen WT, Yingling JM.
J Med Chem (2006) 49 : 2138 -2142
PubMed 16539403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.53 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204170 1 7.50
CHEMBL382838 1 7.38
CHEMBL261454 1 7.09
CHEMBL204966 1 7.02
CHEMBL441176 1 6.86
CHEMBL377711 1 6.82
CHEMBL206233 1 6.60
CHEMBL381532 1 6.56
CHEMBL203791 1 6.56
CHEMBL204063 1 6.43
CHEMBL203619 1 6.43
CHEMBL378167 1 6.07
CHEMBL204139 1 6.06
CHEMBL202730 1 6.00
CHEMBL203214 1 5.79
CHEMBL204158 1 5.33
CHEMBL202625 1 -
CHEMBL427211 1 -
CHEMBL377717 1 -
CHEMBL204061 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204170 IC50 = 32.0 nM 7.50
CHEMBL382838 IC50 = 42.0 nM 7.38
CHEMBL261454 IC50 = 81.0 nM 7.09
CHEMBL204966 IC50 = 96.0 nM 7.02
CHEMBL441176 IC50 = 139.0 nM 6.86
CHEMBL377711 IC50 = 150.0 nM 6.82
CHEMBL206233 IC50 = 249.0 nM 6.60
CHEMBL381532 IC50 = 277.0 nM 6.56
CHEMBL203791 IC50 = 274.0 nM 6.56
CHEMBL204063 IC50 = 371.0 nM 6.43
CHEMBL203619 IC50 = 371.0 nM 6.43
CHEMBL378167 IC50 = 854.0 nM 6.07
CHEMBL204139 IC50 = 872.0 nM 6.06
CHEMBL202730 IC50 = 1001.0 nM 6.00
CHEMBL203214 IC50 = 1622.0 nM 5.79
CHEMBL204158 IC50 = 4700.0 nM 5.33
CHEMBL202625 IC50 - -
CHEMBL427211 IC50 - -
CHEMBL377717 IC50 - -
CHEMBL204061 IC50 - -