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Assay Detail

CHEMBL5579408

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

Binding
Inhibition of STT3A/STT3B mediated N-linked glycosylation in human H1-HeLa cells stably transduced with ERluc by measuring effective concentration of inhibition incubated for 18 hrs by One-Glo luciferase reporter assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H1-HeLa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Potent STT3A/B Inhibitors and Assessment of Their Multipathogen Antiviral Potential and Safety.
Pero JE, Mueller EA, Adams AM, Adolph RS, Bagchi P, Balce D, Bantscheff M, Barauskas O, Bartha I, Bohan D, Cai H, Carabajal E, Cassidy J, Cato M, Chaudhary KW, Chen D, Chen YP, Colas C, Darwech I, Eberl HC, Fernandez B, Gordon E, Grosse J, Hansen J, Hetzler B, Hwang S, Jeyasingh S, Kowalski B, Lehmann S, Lo G, McAllaster M, McHugh C, Momont C, Newby Z, Nigro M, Oladunni F, Pannirselvam M, Park A, Pearson N, Peat AJ, Plastridge B, Ranjan R, Safabakhsh P, Shapiro ND, Soriaga L, Stokes N, Sweeney D, Talecki L, Telenti A, Terrell A, Tse W, Wang L, Wang S, Wedel L, Werner T, Dalmas Wilk D, Yim S, Zhou J.
J Med Chem (2024) 67 : 14586 -14608
PubMed 39136957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.96 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5583975 1 9.00
CHEMBL5595779 1 8.70
CHEMBL5583748 1 8.30
CHEMBL5592276 1 8.30
CHEMBL5584184 1 7.82
CHEMBL5583722 1 7.68
CHEMBL5591147 1 7.64
CHEMBL5593281 1 7.51
CHEMBL5595895 1 7.50
CHEMBL5589992 1 7.44
CHEMBL5592540 1 7.21
CHEMBL5593163 1 6.97
CHEMBL5595968 1 6.76
CHEMBL5595888 1 6.55
CHEMBL5591248 1 6.48
CHEMBL5594134 1 6.41
CHEMBL5593573 1 6.39
CHEMBL5595336 1 6.29
CHEMBL1720448 1 6.23
CHEMBL5590333 1 6.21
CHEMBL5579784 1 6.11
CHEMBL5590068 1 6.08
CHEMBL5592058 1 5.86
CHEMBL5583718 1 5.36
CHEMBL1897966 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5583975 EC50 = 1.0 nM 9.00
CHEMBL5595779 EC50 = 2.0 nM 8.70
CHEMBL5583748 EC50 = 5.0 nM 8.30
CHEMBL5592276 EC50 = 5.0 nM 8.30
CHEMBL5584184 EC50 = 15.0 nM 7.82
CHEMBL5583722 EC50 = 21.0 nM 7.68
CHEMBL5591147 EC50 = 23.0 nM 7.64
CHEMBL5593281 EC50 = 31.0 nM 7.51
CHEMBL5595895 EC50 = 32.0 nM 7.50
CHEMBL5589992 EC50 = 36.0 nM 7.44
CHEMBL5592540 EC50 = 62.0 nM 7.21
CHEMBL5593163 EC50 = 107.0 nM 6.97
CHEMBL5595968 EC50 = 172.0 nM 6.76
CHEMBL5595888 EC50 = 279.0 nM 6.55
CHEMBL5591248 EC50 = 332.0 nM 6.48
CHEMBL5594134 EC50 = 394.0 nM 6.41
CHEMBL5593573 EC50 = 409.0 nM 6.39
CHEMBL5595336 EC50 = 513.0 nM 6.29
CHEMBL1720448 EC50 = 589.0 nM 6.23
CHEMBL5590333 EC50 = 615.0 nM 6.21
CHEMBL5579784 EC50 = 779.0 nM 6.11
CHEMBL5590068 EC50 = 827.0 nM 6.08
CHEMBL5592058 EC50 = 1390.0 nM 5.86
CHEMBL5583718 EC50 = 4420.0 nM 5.36
CHEMBL1897966 EC50 = 5011.0 nM 5.30