Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1771981

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

Binding
Inhibition of human transglutaminase 2 using Cbz-Gln-Gly as a substrate by GDH-coupled assay
ChEMBL ↗
71
Total Activities
54
Compounds Tested
2
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

Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2.
Klöck C, Jin X, Choi K, Khosla C, Madrid PB, Spencer A, Raimundo BC, Boardman P, Lanza G, Griffin JH.
Bioorg Med Chem Lett (2011) 21 : 2692 -2696
PubMed 21215619 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.43 6.16
Ki 17 5.44 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1770539 — — 2 6.40
CHEMBL1770531 — — 2 6.39
CHEMBL1770519 — — 1 6.16
CHEMBL1770394 — — 2 6.16
CHEMBL1770520 — — 1 6.10
CHEMBL1770529 — — 1 6.10
CHEMBL1770521 — — 1 6.05
CHEMBL1770154 — — 2 6.05
CHEMBL1770395 — — 2 6.05
CHEMBL1770522 — — 1 6.00
CHEMBL1770528 — — 1 6.00
CHEMBL1770525 — — 1 5.96
CHEMBL1770523 — — 1 5.96
CHEMBL1770399 — — 1 5.96
CHEMBL1770536 — — 1 5.96
CHEMBL1770537 — — 1 5.92
CHEMBL1770400 — — 1 5.92
CHEMBL1770533 — — 1 5.89
CHEMBL1770527 — — 1 5.85
CHEMBL1770524 — — 1 5.85
CHEMBL1770401 — — 1 5.85
CHEMBL1770517 — — 1 5.85
CHEMBL1770532 — — 1 5.82
CHEMBL1770545 — — 1 5.82
CHEMBL1770535 — — 1 5.75
CHEMBL1770544 — — 2 5.68
CHEMBL1770530 — — 1 5.68
CHEMBL1770518 — — 2 5.55
CHEMBL1770547 — — 1 5.54
CHEMBL1770541 — — 2 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1770539 — Ki = 400.0 nM 6.40
CHEMBL1770531 — Ki = 410.0 nM 6.39
CHEMBL1770519 — IC50 = 700.0 nM 6.16
CHEMBL1770394 — Ki = 700.0 nM 6.16
CHEMBL1770529 — IC50 = 800.0 nM 6.10
CHEMBL1770520 — IC50 = 800.0 nM 6.10
CHEMBL1770539 — IC50 = 900.0 nM 6.05
CHEMBL1770395 — Ki = 900.0 nM 6.05
CHEMBL1770154 — IC50 = 900.0 nM 6.05
CHEMBL1770521 — IC50 = 900.0 nM 6.05
CHEMBL1770528 — IC50 = 1000.0 nM 6.00
CHEMBL1770522 — IC50 = 1000.0 nM 6.00
CHEMBL1770523 — IC50 = 1100.0 nM 5.96
CHEMBL1770536 — IC50 = 1100.0 nM 5.96
CHEMBL1770399 — IC50 = 1100.0 nM 5.96
CHEMBL1770525 — IC50 = 1100.0 nM 5.96
CHEMBL1770400 — IC50 = 1200.0 nM 5.92
CHEMBL1770537 — IC50 = 1200.0 nM 5.92
CHEMBL1770533 — IC50 = 1300.0 nM 5.89
CHEMBL1770154 — Ki = 1300.0 nM 5.89
CHEMBL1770401 — IC50 = 1400.0 nM 5.85
CHEMBL1770517 — IC50 = 1400.0 nM 5.85
CHEMBL1770524 — IC50 = 1400.0 nM 5.85
CHEMBL1770527 — IC50 = 1400.0 nM 5.85
CHEMBL1770545 — IC50 = 1500.0 nM 5.82
CHEMBL1770394 — IC50 = 1500.0 nM 5.82
CHEMBL1770532 — IC50 = 1500.0 nM 5.82
CHEMBL1770531 — IC50 = 1500.0 nM 5.82
CHEMBL1770535 — IC50 = 1800.0 nM 5.75
CHEMBL1770544 — IC50 = 2100.0 nM 5.68
CHEMBL1770530 — IC50 = 2100.0 nM 5.68
CHEMBL1770518 — IC50 = 2800.0 nM 5.55
CHEMBL1770547 — IC50 = 2900.0 nM 5.54
CHEMBL1770541 — Ki = 3000.0 nM 5.52
CHEMBL1770389 — Ki = 3000.0 nM 5.52
CHEMBL1770518 — Ki = 3300.0 nM 5.48
CHEMBL1770397 — IC50 = 3600.0 nM 5.44
CHEMBL1770526 — Ki = 4000.0 nM 5.40
CHEMBL1770526 — IC50 = 4000.0 nM 5.40
CHEMBL1770395 — IC50 = 4300.0 nM 5.37
CHEMBL1770398 — IC50 = 4700.0 nM 5.33
CHEMBL1770541 — IC50 = 4800.0 nM 5.32
CHEMBL1770544 — Ki = 5300.0 nM 5.28
CHEMBL1770396 — Ki = 5400.0 nM 5.27
CHEMBL1770534 — IC50 = 5500.0 nM 5.26
CHEMBL1770540 — IC50 = 6000.0 nM 5.22
CHEMBL1770542 — IC50 = 6300.0 nM 5.20
CHEMBL1770546 — IC50 = 7300.0 nM 5.14
CHEMBL1770543 — IC50 = 7900.0 nM 5.10
CHEMBL515155 ISOINDIGO IC50 = 8000.0 nM 5.10