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Assay Detail

CHEMBL3582891

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

Binding
Inhibition of recombinant human placental AdoHcy hydrolase expressed in Escherichia coli BL21 using AdoHcy as substrate preincubated for 10 mins followed by substrate addition measured after 20 mins by DTNB coupled 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

Adenosylhomocysteinase (CHEMBL2664)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationships of Neplanocin A Analogues as S-Adenosylhomocysteine Hydrolase Inhibitors and Their Antiviral and Antitumor Activities.
Chandra G, Moon YW, Lee Y, Jang JY, Song J, Nayak A, Oh K, Mulamoottil VA, Sahu PK, Kim G, Chang TS, Noh M, Lee SK, Choi S, Jeong LS.
J Med Chem (2015) 58 : 5108 -5120
PubMed 26010585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.18 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64718 FLUORO-NEPLANOCIN A 1 6.62
CHEMBL154745 1 6.36
CHEMBL8771 NEOPLANOCIN A 1 6.33
CHEMBL310547 1 6.32
CHEMBL3580900 1 6.04
CHEMBL80375 1 5.42
CHEMBL200935 DEAZANEPLANOCIN A 1 -
CHEMBL3580894 1 -
CHEMBL3580895 1 -
CHEMBL3580896 1 -
CHEMBL3580897 1 -
CHEMBL3580898 1 -
CHEMBL3580899 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64718 FLUORO-NEPLANOCIN A IC50 = 240.0 nM 6.62
CHEMBL154745 IC50 = 440.0 nM 6.36
CHEMBL8771 NEOPLANOCIN A IC50 = 470.0 nM 6.33
CHEMBL310547 IC50 = 480.0 nM 6.32
CHEMBL3580900 IC50 = 910.0 nM 6.04
CHEMBL80375 IC50 = 3760.0 nM 5.42
CHEMBL200935 DEAZANEPLANOCIN A IC50 > 100000.0 nM -
CHEMBL3580894 IC50 > 100000.0 nM -
CHEMBL3580895 IC50 > 100000.0 nM -
CHEMBL3580896 IC50 > 100000.0 nM -
CHEMBL3580897 IC50 > 100000.0 nM -
CHEMBL3580898 IC50 > 100000.0 nM -
CHEMBL3580899 IC50 > 100000.0 nM -