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Assay Detail

CHEMBL4258356

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Binding
Inhibition of full-length GST-fused human CBS assessed as reduction in H2S production using 2 mM S-methylcysteine as substrate preincubated for 3 mins followed by substrate addition
2
Total Activities
2
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

Cystathionine beta-synthase (CHEMBL3399911)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer <i>in vitro</i> and <i>in vivo</i>.
Niu W, Chen F, Wang J, Qian J, Yan S.
Medchemcomm (2018) 9 : 113 -120
PubMed 30108905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.59 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1172216 SIKOKIANIN C 1 6.05
CHEMBL347862 CARBOXYMETHOXYLAMINE 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1172216 SIKOKIANIN C IC50 = 900.0 nM 6.05
CHEMBL347862 CARBOXYMETHOXYLAMINE IC50 = 7500.0 nM 5.12