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Assay Detail

CHEMBL5036223

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

Binding
Modulation of CD33 pre-mRNA splicing in human K562 cells assessed as induction of exon 2 skipping measured after 18 to 24 hrs by Nano-Luciferase reporter assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators.
Chappie TA, Abdelmessih M, Ambroise CW, Boehm M, Cai M, Green M, Guilmette E, Steppan CM, Stevens LM, Wei L, Xi S, Hasson SA.
ACS Med Chem Lett (2022) 13 : 55 -62
PubMed 35059124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.50 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4130157 1 6.24
CHEMBL4114159 1 5.85
CHEMBL4108330 1 5.44
CHEMBL4107804 1 5.43
CHEMBL4126496 1 5.36
CHEMBL4109308 1 5.35
CHEMBL4126072 1 5.25
CHEMBL5088467 1 5.11
CHEMBL4127458 1 -
CHEMBL4127311 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4130157 EC50 = 580.0 nM 6.24
CHEMBL4114159 EC50 = 1400.0 nM 5.85
CHEMBL4108330 EC50 = 3600.0 nM 5.44
CHEMBL4107804 EC50 = 3700.0 nM 5.43
CHEMBL4126496 EC50 = 4400.0 nM 5.36
CHEMBL4109308 EC50 = 4500.0 nM 5.35
CHEMBL4126072 EC50 = 5600.0 nM 5.25
CHEMBL5088467 EC50 = 7800.0 nM 5.11
CHEMBL4127458 EC50 > 10000.0 nM -
CHEMBL4127311 EC50 > 10000.0 nM -