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Assay Detail

CHEMBL5032404

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

Binding
Inhibition of recombinant human NO66 expressed in Escherichia coli BL21 (DE3) using RPL8 N205PVEHPFGGGNHQHIGKPST224 as substrate preincubated for 15 mins followed by substrate addition and measured after 30 to 60 mins by RapidFire Mass spectrometry assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 16 4.69 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316034 1 6.96
CHEMBL90852 N-OXALYLGLYCINE 1 5.46
CHEMBL5089880 1 4.64
CHEMBL5081435 1 4.63
CHEMBL5070745 1 4.43
CHEMBL1230640 1 4.42
CHEMBL5089117 1 4.40
CHEMBL5076580 1 4.32
CHEMBL5084638 1 4.14
CHEMBL5071515 1 4.10
CHEMBL5071002 1 4.09
CHEMBL5080728 1 -
CHEMBL5083418 1 -
CHEMBL5091848 1 -
CHEMBL5072902 1 -
CHEMBL5084143 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316034 IC50 = 110.0 nM 6.96
CHEMBL90852 N-OXALYLGLYCINE IC50 = 3500.0 nM 5.46
CHEMBL5089880 IC50 = 22900.0 nM 4.64
CHEMBL5081435 IC50 = 23500.0 nM 4.63
CHEMBL5070745 IC50 = 36900.0 nM 4.43
CHEMBL1230640 IC50 = 38500.0 nM 4.42
CHEMBL5089117 IC50 = 40200.0 nM 4.40
CHEMBL5076580 IC50 = 48000.0 nM 4.32
CHEMBL5084638 IC50 = 71700.0 nM 4.14
CHEMBL5071515 IC50 = 80200.0 nM 4.10
CHEMBL5071002 IC50 = 81200.0 nM 4.09
CHEMBL5080728 IC50 > 200000.0 nM -
CHEMBL5083418 IC50 = 163000.0 nM -
CHEMBL5091848 IC50 > 200000.0 nM -
CHEMBL5072902 IC50 = 182000.0 nM -
CHEMBL5084143 IC50 = 100400.0 nM -