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Assay Detail

CHEMBL930571

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Binding
Inhibition of GRE-mediated transcription in human HepG cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural analogs of tylophora alkaloids may not be functional analogs.
Gao W, Chen AP, Leung CH, Gullen EA, Fürstner A, Shi Q, Wei L, Lee KH, Cheng YC.
Bioorg Med Chem Lett (2008) 18 : 704 -709
PubMed 18077159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.91 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270213 1 8.00
CHEMBL228286 (-)-ANTOFINE 1 7.62
CHEMBL250426 (S)-TYLOPHORINE 1 6.64
CHEMBL258137 TYLOPHORINE 1 6.27
CHEMBL255848 1 5.61
CHEMBL270214 1 5.35
CHEMBL231290 1 5.14
CHEMBL231192 1 5.04
CHEMBL395994 1 4.72
CHEMBL395996 1 4.68
CHEMBL403878 1 -
CHEMBL231193 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270213 IC50 = 10.0 nM 8.00
CHEMBL228286 (-)-ANTOFINE IC50 = 24.0 nM 7.62
CHEMBL250426 (S)-TYLOPHORINE IC50 = 229.0 nM 6.64
CHEMBL258137 TYLOPHORINE IC50 = 534.0 nM 6.27
CHEMBL255848 IC50 = 2440.0 nM 5.61
CHEMBL270214 IC50 = 4500.0 nM 5.35
CHEMBL231290 IC50 = 7200.0 nM 5.14
CHEMBL231192 IC50 = 9200.0 nM 5.04
CHEMBL395994 IC50 = 19000.0 nM 4.72
CHEMBL395996 IC50 = 20700.0 nM 4.68
CHEMBL403878 IC50 > 15000.0 nM -
CHEMBL231193 IC50 > 30000.0 nM -