Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5032402

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

Binding
Inhibition of human FIH using HLEVVKLLLEAGADVNAQDK-CONH2 as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by RapidFire Mass spectrometry assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hypoxia-inducible factor 1-alpha inhibitor (CHEMBL5909)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53.
Nowak RP, Tumber A, Hendrix E, Ansari MSZ, Sabatino M, Antonini L, Andrijes R, Salah E, Mautone N, Pellegrini FR, Simelis K, Kawamura A, Johansson C, Passeri D, Pellicciari R, Ciogli A, Del Bufalo D, Ragno R, Coleman ML, Trisciuoglio D, Mai A, Oppermann U, Schofield CJ, Rotili D.
J Med Chem (2021) 64 : 17031 -17050
PubMed 34843649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.75 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5091848 1 5.40
CHEMBL5072902 1 5.11
CHEMBL5071002 1 4.98
CHEMBL5089117 1 4.82
CHEMBL5083418 1 4.80
CHEMBL5089880 1 4.72
CHEMBL5081435 1 4.71
CHEMBL5076580 1 4.70
CHEMBL5084638 1 4.62
CHEMBL5070745 1 4.53
CHEMBL5071515 1 4.52
CHEMBL5084143 1 4.06
CHEMBL5080728 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5091848 IC50 = 4000.0 nM 5.40
CHEMBL5072902 IC50 = 7800.0 nM 5.11
CHEMBL5071002 IC50 = 10500.0 nM 4.98
CHEMBL5089117 IC50 = 15300.0 nM 4.82
CHEMBL5083418 IC50 = 15900.0 nM 4.80
CHEMBL5089880 IC50 = 19200.0 nM 4.72
CHEMBL5081435 IC50 = 19400.0 nM 4.71
CHEMBL5076580 IC50 = 20200.0 nM 4.70
CHEMBL5084638 IC50 = 23800.0 nM 4.62
CHEMBL5070745 IC50 = 29800.0 nM 4.53
CHEMBL5071515 IC50 = 30100.0 nM 4.52
CHEMBL5084143 IC50 = 86600.0 nM 4.06
CHEMBL5080728 IC50 > 100000.0 nM -