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Assay Detail

CHEMBL1055397

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

Functional
Inhibition of hypoxia-induced HIF1alpha protein accumulation in human Hep3B cells treated for 30 mins measured after 12 hrs by Western blot analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Hep 3B2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hypoxia-inducible factor 1-alpha (CHEMBL4261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
Dat NT, Jin X, Lee K, Hong YS, Kim YH, Lee JJ.
J Nat Prod (2009) 72 : 39 -43
PubMed 19072214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.23 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205924 MORACIN O 1 9.85
CHEMBL561971 MORACIN P 1 9.19
CHEMBL383824 ALVESPIMYCIN 2.0 1 7.24
CHEMBL563553 MULBERROFURAN H 1 6.85
CHEMBL525084 SANGGENON O 1 5.99
CHEMBL204813 SANGGENON C 1 5.90
CHEMBL445265 MULBERROFURAN G 1 5.58
CHEMBL570526 KUWANON R 1 5.50
CHEMBL564896 ALBAFURAN A 1 5.46
CHEMBL562810 MULBERROFURAN W 1 5.44
CHEMBL2368640 1 5.42
CHEMBL517247 MULBERROFURAN D 1 5.39
CHEMBL570475 KUWANON J 1 5.39
CHEMBL562169 MORACIN Q 1 5.23
CHEMBL570609 KUWANON V 1 5.08
CHEMBL512578 MORACIN M 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205924 MORACIN O IC50 = 0.14 nM 9.85
CHEMBL561971 MORACIN P IC50 = 0.65 nM 9.19
CHEMBL383824 ALVESPIMYCIN IC50 = 57.2 nM 7.24
CHEMBL563553 MULBERROFURAN H IC50 = 140.0 nM 6.85
CHEMBL525084 SANGGENON O IC50 = 1030.0 nM 5.99
CHEMBL204813 SANGGENON C IC50 = 1260.0 nM 5.90
CHEMBL445265 MULBERROFURAN G IC50 = 2600.0 nM 5.58
CHEMBL570526 KUWANON R IC50 = 3170.0 nM 5.50
CHEMBL564896 ALBAFURAN A IC50 = 3510.0 nM 5.46
CHEMBL562810 MULBERROFURAN W IC50 = 3620.0 nM 5.44
CHEMBL2368640 IC50 = 3800.0 nM 5.42
CHEMBL517247 MULBERROFURAN D IC50 = 4050.0 nM 5.39
CHEMBL570475 KUWANON J IC50 = 4100.0 nM 5.39
CHEMBL562169 MORACIN Q IC50 = 5880.0 nM 5.23
CHEMBL570609 KUWANON V IC50 = 8320.0 nM 5.08
CHEMBL512578 MORACIN M IC50 > 50000.0 nM -