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Assay Detail

CHEMBL928263

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

Functional
Antiproliferative activity against mouse NIH3T3 cells by [3H]thymidine assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 1 — Organism
Curated By Autocuration

Target

NIH3T3 (CHEMBL614822)
Type CELL-LINE
Organism Mus musculus

Publication

Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD, Britt KS, Huss KL, Voss MD, Wang Y, Clawson DK, Yingling JM, Sawyer JS.
J Med Chem (2008) 51 : 2302 -2306
PubMed 18314943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.67 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406411 1 7.70
CHEMBL411855 1 7.29
CHEMBL409331 1 7.27
CHEMBL411297 1 7.14
CHEMBL261454 1 7.09
CHEMBL261674 1 7.04
CHEMBL409525 1 7.01
CHEMBL261762 1 7.01
CHEMBL260015 1 6.68
CHEMBL409158 1 6.60
CHEMBL260240 1 6.59
CHEMBL260923 1 6.47
CHEMBL260147 1 6.38
CHEMBL409356 1 6.14
CHEMBL411741 1 5.99
CHEMBL410308 1 5.64
CHEMBL261702 1 5.29
CHEMBL260239 1 -
CHEMBL261625 1 -
CHEMBL408181 1 -
CHEMBL409515 1 -
CHEMBL259169 1 -
CHEMBL258964 1 -
CHEMBL261701 1 -
CHEMBL406407 1 -
CHEMBL260729 1 -
CHEMBL258641 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406411 IC50 = 20.0 nM 7.70
CHEMBL411855 IC50 = 51.0 nM 7.29
CHEMBL409331 IC50 = 54.0 nM 7.27
CHEMBL411297 IC50 = 72.0 nM 7.14
CHEMBL261454 IC50 = 81.0 nM 7.09
CHEMBL261674 IC50 = 92.0 nM 7.04
CHEMBL409525 IC50 = 98.0 nM 7.01
CHEMBL261762 IC50 = 97.0 nM 7.01
CHEMBL260015 IC50 = 210.0 nM 6.68
CHEMBL409158 IC50 = 250.0 nM 6.60
CHEMBL260240 IC50 = 254.0 nM 6.59
CHEMBL260923 IC50 = 338.0 nM 6.47
CHEMBL260147 IC50 = 420.0 nM 6.38
CHEMBL409356 IC50 = 730.0 nM 6.14
CHEMBL411741 IC50 = 1030.0 nM 5.99
CHEMBL410308 IC50 = 2270.0 nM 5.64
CHEMBL261702 IC50 = 5100.0 nM 5.29
CHEMBL260239 IC50 - -
CHEMBL261625 IC50 > 20000.0 nM -
CHEMBL408181 IC50 - -
CHEMBL409515 IC50 - -
CHEMBL259169 IC50 - -
CHEMBL258964 IC50 - -
CHEMBL261701 IC50 > 20000.0 nM -
CHEMBL406407 IC50 > 20000.0 nM -
CHEMBL260729 IC50 - -
CHEMBL258641 IC50 - -