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Assay Detail

CHEMBL1006266

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

Binding
Destabilizing effect on human recombinant PHD2 (181-426) expressed in Escherichia coli BL21 (DE3) assessed as half life by limited trypsinolysis/MALDI-MS analysis in presence of ferrous ion
7
Total Activities
7
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

Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure.
Stubbs CJ, Loenarz C, Mecinović J, Yeoh KK, Hindley N, Liénard BM, Sobott F, Schofield CJ, Flashman E.
J Med Chem (2009) 52 : 2799 -2805
PubMed 19364117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.45 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426560 1 7.14
CHEMBL485022 1 6.29
CHEMBL316034 1 5.72
CHEMBL90852 N-OXALYLGLYCINE 1 4.73
CHEMBL503160 FUMARIC ACID 3.0 1 4.72
CHEMBL576 SUCCINIC ACID 3.0 1 4.07
CHEMBL485023 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426560 IC50 = 73.0 nM 7.14
CHEMBL485022 IC50 = 512.0 nM 6.29
CHEMBL316034 IC50 = 1910.0 nM 5.72
CHEMBL90852 N-OXALYLGLYCINE IC50 = 18500.0 nM 4.73
CHEMBL503160 FUMARIC ACID IC50 = 19090.0 nM 4.72
CHEMBL576 SUCCINIC ACID IC50 = 85300.0 nM 4.07
CHEMBL485023 IC50 = 230000.0 nM -