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Assay Detail

CHEMBL1066254

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

Binding
Inhibition of guinea pig liver transglutaminase
141
Total Activities
141
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-glutamine gamma-glutamyltransferase (CHEMBL3308976)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones.
Ozaki S, Ebisui E, Hamada K, Goto J, Suzuki AZ, Terauchi A, Mikoshiba K.
Bioorg Med Chem Lett (2010) 20 : 1141 -1144
PubMed 20053561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 141 5.56 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL598522 1 7.09
CHEMBL597916 1 7.00
CHEMBL610215 1 6.92
CHEMBL598521 1 6.72
CHEMBL598529 1 6.68
CHEMBL611979 1 6.64
CHEMBL597079 1 6.50
CHEMBL597103 1 6.50
CHEMBL589994 1 6.44
CHEMBL598319 1 6.38
CHEMBL597917 1 6.38
CHEMBL599534 1 6.36
CHEMBL599729 1 6.33
CHEMBL599107 1 6.28
CHEMBL582295 1 6.26
CHEMBL608737 1 6.24
CHEMBL599555 1 6.23
CHEMBL611978 1 6.21
CHEMBL590246 1 6.19
CHEMBL598910 1 6.17
CHEMBL599350 1 6.17
CHEMBL609903 1 6.16
CHEMBL602665 1 6.11
CHEMBL590249 1 6.10
CHEMBL600082 1 6.08
CHEMBL599730 1 6.08
CHEMBL598051 1 6.08
CHEMBL611080 1 6.07
CHEMBL590493 1 6.04
CHEMBL602862 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL598522 IC50 = 81.0 nM 7.09
CHEMBL597916 IC50 = 100.0 nM 7.00
CHEMBL610215 IC50 = 120.0 nM 6.92
CHEMBL598521 IC50 = 190.0 nM 6.72
CHEMBL598529 IC50 = 210.0 nM 6.68
CHEMBL611979 IC50 = 230.0 nM 6.64
CHEMBL597103 IC50 = 320.0 nM 6.50
CHEMBL597079 IC50 = 320.0 nM 6.50
CHEMBL589994 IC50 = 360.0 nM 6.44
CHEMBL597917 IC50 = 420.0 nM 6.38
CHEMBL598319 IC50 = 420.0 nM 6.38
CHEMBL599534 IC50 = 440.0 nM 6.36
CHEMBL599729 IC50 = 470.0 nM 6.33
CHEMBL599107 IC50 = 530.0 nM 6.28
CHEMBL582295 IC50 = 550.0 nM 6.26
CHEMBL608737 IC50 = 570.0 nM 6.24
CHEMBL599555 IC50 = 590.0 nM 6.23
CHEMBL611978 IC50 = 610.0 nM 6.21
CHEMBL590246 IC50 = 650.0 nM 6.19
CHEMBL599350 IC50 = 680.0 nM 6.17
CHEMBL598910 IC50 = 670.0 nM 6.17
CHEMBL609903 IC50 = 700.0 nM 6.16
CHEMBL602665 IC50 = 770.0 nM 6.11
CHEMBL590249 IC50 = 800.0 nM 6.10
CHEMBL598051 IC50 = 840.0 nM 6.08
CHEMBL600082 IC50 = 830.0 nM 6.08
CHEMBL599730 IC50 = 830.0 nM 6.08
CHEMBL611080 IC50 = 850.0 nM 6.07
CHEMBL590493 IC50 = 920.0 nM 6.04
CHEMBL602862 IC50 = 980.0 nM 6.01
CHEMBL598239 IC50 = 1000.0 nM 6.00
CHEMBL608730 IC50 = 1000.0 nM 6.00
CHEMBL596661 IC50 = 1100.0 nM 5.96
CHEMBL598240 IC50 = 1100.0 nM 5.96
CHEMBL600659 IC50 = 1200.0 nM 5.92
CHEMBL601264 IC50 = 1200.0 nM 5.92
CHEMBL590731 IC50 = 1200.0 nM 5.92
CHEMBL609894 IC50 = 1300.0 nM 5.89
CHEMBL597178 IC50 = 1400.0 nM 5.85
CHEMBL598718 IC50 = 1400.0 nM 5.85
CHEMBL597511 IC50 = 1400.0 nM 5.85
CHEMBL597714 IC50 = 1400.0 nM 5.85
CHEMBL607563 IC50 = 1400.0 nM 5.85
CHEMBL599535 IC50 = 1400.0 nM 5.85
CHEMBL609631 IC50 = 1400.0 nM 5.85
CHEMBL597918 IC50 = 1500.0 nM 5.82
CHEMBL598084 IC50 = 1500.0 nM 5.82
CHEMBL598905 IC50 = 1500.0 nM 5.82
CHEMBL598114 IC50 = 1700.0 nM 5.77
CHEMBL598701 IC50 = 1700.0 nM 5.77