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Assay Detail

CHEMBL5339817

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

Binding
Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5'P-uacacucgaucuggacuaaagcugcuc-3' and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

METTL3/METTL14 (CHEMBL4106140)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey.
Fiorentino F, Menna M, Rotili D, Valente S, Mai A.
J Med Chem (2023) 66 : 1654 -1677
PubMed 36692498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.02 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5396973 1 8.44
CHEMBL5405105 1 8.36
CHEMBL5082807 1 8.21
CHEMBL5417468 1 8.21
CHEMBL5410561 1 8.21
CHEMBL5398269 1 8.21
CHEMBL5415737 1 8.21
CHEMBL5075067 1 8.21
CHEMBL5080742 1 8.21
CHEMBL5091295 1 8.21
CHEMBL5092868 1 8.21
CHEMBL5083389 1 8.21
CHEMBL5418009 1 8.21
CHEMBL5423125 1 8.21
CHEMBL5405396 1 8.21
CHEMBL5405801 1 8.21
CHEMBL5419185 1 8.21
CHEMBL5402970 1 8.10
CHEMBL5288865 1 4.29
CHEMBL5411328 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5396973 IC50 = 3.63 nM 8.44
CHEMBL5405105 IC50 = 4.35 nM 8.36
CHEMBL5082807 IC50 = 6.1 nM 8.21
CHEMBL5417468 IC50 = 6.1 nM 8.21
CHEMBL5410561 IC50 = 6.1 nM 8.21
CHEMBL5398269 IC50 = 6.1 nM 8.21
CHEMBL5415737 IC50 = 6.1 nM 8.21
CHEMBL5075067 IC50 = 6.1 nM 8.21
CHEMBL5080742 IC50 = 6.1 nM 8.21
CHEMBL5091295 IC50 = 6.1 nM 8.21
CHEMBL5092868 IC50 = 6.1 nM 8.21
CHEMBL5083389 IC50 = 6.1 nM 8.21
CHEMBL5418009 IC50 = 6.1 nM 8.21
CHEMBL5423125 IC50 = 6.1 nM 8.21
CHEMBL5405396 IC50 = 6.1 nM 8.21
CHEMBL5405801 IC50 = 6.22 nM 8.21
CHEMBL5419185 IC50 = 6.1 nM 8.21
CHEMBL5402970 IC50 = 7.9 nM 8.10
CHEMBL5288865 IC50 = 51700.0 nM 4.29
CHEMBL5411328 IC50 < 6.0 nM -