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Assay Detail

CHEMBL4714988

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

Functional
Inhibition of Activin A-induced Smad3 phosphorylation in human Epi293F cells pretreated for 10 mins followed by addition of TGF-beta1 measured after 120 mins by AlphaLISA assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Epi293F
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Selective Transforming Growth Factor β Type II Receptor Inhibitors as Antifibrosis Agents.
Miwa S,Yokota M,Ueyama Y,Maeda K,Ogoshi Y,Seki N,Ogawa N,Nishihata J,Nomura A,Adachi T,Kitao Y,Nozawa K,Ishikawa T,Ukaji Y,Shiozaki M
ACS Med Chem Lett (2021) 12 : 745 -751
PubMed 34055221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.40 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4744618 1 6.41
CHEMBL4758580 1 6.37
CHEMBL4752410 1 6.28
CHEMBL4764221 1 6.20
CHEMBL4791414 1 6.06
CHEMBL4747422 1 6.04
CHEMBL4792464 1 5.66
CHEMBL4751832 1 5.54
CHEMBL4747912 1 5.48
CHEMBL4741913 1 5.39
CHEMBL4752199 1 5.32
CHEMBL4750258 1 5.12
CHEMBL4779273 1 5.04
CHEMBL4741185 1 4.96
CHEMBL4748097 1 4.92
CHEMBL4744988 1 4.92
CHEMBL4764416 1 4.92
CHEMBL4795223 1 4.85
CHEMBL4749061 1 4.82
CHEMBL4779579 1 4.66
CHEMBL4798505 1 4.54
CHEMBL4792978 1 -
CHEMBL4787891 1 -
CHEMBL4749011 1 -
CHEMBL4763627 1 -
CHEMBL4782729 1 -
CHEMBL4763122 1 -
CHEMBL4777071 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4744618 IC50 = 390.0 nM 6.41
CHEMBL4758580 IC50 = 430.0 nM 6.37
CHEMBL4752410 IC50 = 520.0 nM 6.28
CHEMBL4764221 IC50 = 630.0 nM 6.20
CHEMBL4791414 IC50 = 870.0 nM 6.06
CHEMBL4747422 IC50 = 920.0 nM 6.04
CHEMBL4792464 IC50 = 2200.0 nM 5.66
CHEMBL4751832 IC50 = 2900.0 nM 5.54
CHEMBL4747912 IC50 = 3300.0 nM 5.48
CHEMBL4741913 IC50 = 4100.0 nM 5.39
CHEMBL4752199 IC50 = 4800.0 nM 5.32
CHEMBL4750258 IC50 = 7600.0 nM 5.12
CHEMBL4779273 IC50 = 9100.0 nM 5.04
CHEMBL4741185 IC50 = 11000.0 nM 4.96
CHEMBL4748097 IC50 = 12000.0 nM 4.92
CHEMBL4744988 IC50 = 12000.0 nM 4.92
CHEMBL4764416 IC50 = 12000.0 nM 4.92
CHEMBL4795223 IC50 = 14000.0 nM 4.85
CHEMBL4749061 IC50 = 15000.0 nM 4.82
CHEMBL4779579 IC50 = 22000.0 nM 4.66
CHEMBL4798505 IC50 = 29000.0 nM 4.54
CHEMBL4792978 IC50 > 38000.0 nM -
CHEMBL4787891 IC50 > 1300.0 nM -
CHEMBL4749011 IC50 > 38000.0 nM -
CHEMBL4763627 IC50 > 38000.0 nM -
CHEMBL4782729 IC50 > 38000.0 nM -
CHEMBL4763122 IC50 > 3800.0 nM -
CHEMBL4777071 IC50 > 3800.0 nM -