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Assay Detail

CHEMBL3424618

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

Binding
Inhibition of transglutaminase 2 (unknown origin)
12
Total Activities
12
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

(±) cis-Bisamido epoxides: A novel series of potent FXIII-A inhibitors.
Avery CA, Pease RJ, Smith K, Boothby M, Buckley HM, Grant PJ, Fishwick CW.
Eur J Med Chem (2015) 98 : 49 -53
PubMed 26005023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.10 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3423198 1 8.02
CHEMBL3423193 1 7.34
CHEMBL3423194 1 7.32
CHEMBL3423202 1 7.32
CHEMBL3423195 1 7.30
CHEMBL3423197 1 7.24
CHEMBL3423200 1 7.06
CHEMBL3423199 1 6.89
CHEMBL3423192 1 6.82
CHEMBL3423203 1 6.82
CHEMBL3423196 1 5.96
CHEMBL3423201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3423198 IC50 = 9.6 nM 8.02
CHEMBL3423193 IC50 = 46.0 nM 7.34
CHEMBL3423194 IC50 = 48.0 nM 7.32
CHEMBL3423202 IC50 = 48.0 nM 7.32
CHEMBL3423195 IC50 = 50.0 nM 7.30
CHEMBL3423197 IC50 = 57.0 nM 7.24
CHEMBL3423200 IC50 = 88.0 nM 7.06
CHEMBL3423199 IC50 = 130.0 nM 6.89
CHEMBL3423192 IC50 = 150.0 nM 6.82
CHEMBL3423203 IC50 = 150.0 nM 6.82
CHEMBL3423196 IC50 = 1100.0 nM 5.96
CHEMBL3423201 IC50 - -