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Assay Detail

CHEMBL2155208

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

Binding
Inhibition of human TGM2
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein-glutamine gamma-glutamyltransferase (CHEMBL2730)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease.
Prime ME, Brookfield FA, Courtney SM, Gaines S, Marston RW, Ichihara O, Li M, Vaidya D, Williams H, Pedret-Dunn A, Reed L, Schaertl S, Toledo-Sherman L, Beconi M, Macdonald D, Muñoz-Sanjuan I, Dominguez C, Wityak J.
ACS Med Chem Lett (2012) 3 : 731 -735
PubMed 24900540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.12 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152204 1 6.96
CHEMBL2152105 1 6.85
CHEMBL2152213 1 6.77
CHEMBL2152199 1 6.77
CHEMBL2152214 1 6.75
CHEMBL2152098 1 6.75
CHEMBL2152201 1 6.70
CHEMBL2152099 1 6.70
CHEMBL2152209 1 6.64
CHEMBL2152212 1 6.58
CHEMBL2152207 1 6.55
CHEMBL2152203 1 6.55
CHEMBL2152211 1 6.55
CHEMBL2152090 1 6.55
CHEMBL2152208 1 6.51
CHEMBL2152200 1 6.50
CHEMBL2152197 1 6.44
CHEMBL2152198 1 6.42
CHEMBL2152101 1 6.39
CHEMBL2152103 1 6.34
CHEMBL2152210 1 6.34
CHEMBL2152202 1 6.26
CHEMBL2152102 1 6.21
CHEMBL2152104 1 6.20
CHEMBL2152196 1 6.18
CHEMBL2152100 1 6.11
CHEMBL2152216 1 5.80
CHEMBL2152097 1 5.80
CHEMBL2086885 1 5.54
CHEMBL2152092 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152204 IC50 = 110.0 nM 6.96
CHEMBL2152105 IC50 = 140.0 nM 6.85
CHEMBL2152199 IC50 = 170.0 nM 6.77
CHEMBL2152213 IC50 = 170.0 nM 6.77
CHEMBL2152214 IC50 = 180.0 nM 6.75
CHEMBL2152098 IC50 = 180.0 nM 6.75
CHEMBL2152201 IC50 = 200.0 nM 6.70
CHEMBL2152099 IC50 = 200.0 nM 6.70
CHEMBL2152209 IC50 = 230.0 nM 6.64
CHEMBL2152212 IC50 = 260.0 nM 6.58
CHEMBL2152203 IC50 = 280.0 nM 6.55
CHEMBL2152090 IC50 = 280.0 nM 6.55
CHEMBL2152211 IC50 = 280.0 nM 6.55
CHEMBL2152207 IC50 = 280.0 nM 6.55
CHEMBL2152208 IC50 = 310.0 nM 6.51
CHEMBL2152200 IC50 = 320.0 nM 6.50
CHEMBL2152197 IC50 = 360.0 nM 6.44
CHEMBL2152198 IC50 = 380.0 nM 6.42
CHEMBL2152101 IC50 = 410.0 nM 6.39
CHEMBL2152103 IC50 = 460.0 nM 6.34
CHEMBL2152210 IC50 = 460.0 nM 6.34
CHEMBL2152202 IC50 = 550.0 nM 6.26
CHEMBL2152102 IC50 = 620.0 nM 6.21
CHEMBL2152104 IC50 = 630.0 nM 6.20
CHEMBL2152196 IC50 = 660.0 nM 6.18
CHEMBL2152100 IC50 = 770.0 nM 6.11
CHEMBL2152216 IC50 = 1600.0 nM 5.80
CHEMBL2152097 IC50 = 1600.0 nM 5.80
CHEMBL2086885 IC50 = 2900.0 nM 5.54
CHEMBL2152092 IC50 = 3300.0 nM 5.48
CHEMBL2152091 IC50 = 5100.0 nM 5.29
CHEMBL2152215 IC50 = 8900.0 nM 5.05
CHEMBL2152205 IC50 = 22000.0 nM 4.66
CHEMBL2152096 IC50 = 30000.0 nM 4.52
CHEMBL2152095 IC50 = 55000.0 nM 4.26
CHEMBL2152206 IC50 = 57000.0 nM 4.24
CHEMBL2152094 IC50 > 80000.0 nM -
CHEMBL2152093 IC50 > 80000.0 nM -
CHEMBL2086886 IC50 > 80000.0 nM -