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Assay Detail

CHEMBL4136616

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

Binding
Inhibition of cystathionine gamma-lyase (unknown origin) assessed as reduction in cysteine formation from CPM using L-cystathionine pre-incubated for 15 min followed by L-cystathionine and CPM addition and measured after 7 mins by fluorescence-based primary assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cystathionine gamma-lyase (CHEMBL4295745)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine γ-Lyase (CSE).
Bhattacharjee A, Sinha A, Ratia K, Yin L, Delgado-Rivera L, Petukhov PA, Thatcher GRJ, Wardrop DJ.
ACS Med Chem Lett (2017) 8 : 1241 -1245
PubMed 29259741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.22 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163832 1 5.92
CHEMBL4159854 1 5.72
CHEMBL4166278 1 5.70
CHEMBL4160453 1 5.70
CHEMBL4171052 1 5.70
CHEMBL4162824 1 5.70
CHEMBL4168463 1 5.68
CHEMBL4167775 1 5.60
CHEMBL4166122 1 5.57
CHEMBL4169541 1 5.52
CHEMBL4176894 1 5.52
CHEMBL4170080 1 5.46
CHEMBL4170257 1 5.30
CHEMBL4177072 1 5.30
CHEMBL4173530 1 5.22
CHEMBL4160479 1 5.22
CHEMBL4159631 1 5.22
CHEMBL3318351 1 5.22
CHEMBL4176749 1 5.22
CHEMBL4174491 1 5.22
CHEMBL4159463 1 5.22
CHEMBL4169868 1 5.22
CHEMBL4162997 1 5.16
CHEMBL4161944 1 5.00
CHEMBL4167285 1 5.00
CHEMBL4174098 1 4.92
CHEMBL4166444 1 4.92
CHEMBL4159363 1 4.82
CHEMBL4172146 1 4.82
CHEMBL4173702 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163832 IC50 = 1200.0 nM 5.92
CHEMBL4159854 IC50 = 1900.0 nM 5.72
CHEMBL4166278 IC50 = 2000.0 nM 5.70
CHEMBL4160453 IC50 = 2000.0 nM 5.70
CHEMBL4171052 IC50 = 2000.0 nM 5.70
CHEMBL4162824 IC50 = 2000.0 nM 5.70
CHEMBL4168463 IC50 = 2100.0 nM 5.68
CHEMBL4167775 IC50 = 2500.0 nM 5.60
CHEMBL4166122 IC50 = 2700.0 nM 5.57
CHEMBL4169541 IC50 = 3000.0 nM 5.52
CHEMBL4176894 IC50 = 3000.0 nM 5.52
CHEMBL4170080 IC50 = 3500.0 nM 5.46
CHEMBL4170257 IC50 = 5000.0 nM 5.30
CHEMBL4177072 IC50 = 5000.0 nM 5.30
CHEMBL4173530 IC50 = 6000.0 nM 5.22
CHEMBL4159631 IC50 = 6000.0 nM 5.22
CHEMBL3318351 IC50 = 6000.0 nM 5.22
CHEMBL4176749 IC50 = 6000.0 nM 5.22
CHEMBL4159463 IC50 = 6000.0 nM 5.22
CHEMBL4160479 IC50 = 6000.0 nM 5.22
CHEMBL4169868 IC50 = 6000.0 nM 5.22
CHEMBL4174491 IC50 = 6000.0 nM 5.22
CHEMBL4162997 IC50 = 7000.0 nM 5.16
CHEMBL4161944 IC50 = 10000.0 nM 5.00
CHEMBL4167285 IC50 = 10000.0 nM 5.00
CHEMBL4174098 IC50 = 12000.0 nM 4.92
CHEMBL4166444 IC50 = 12000.0 nM 4.92
CHEMBL4173702 IC50 = 15000.0 nM 4.82
CHEMBL4172146 IC50 = 15000.0 nM 4.82
CHEMBL4159363 IC50 = 15000.0 nM 4.82
CHEMBL4162734 IC50 = 25000.0 nM 4.60
CHEMBL4166176 IC50 = 40000.0 nM 4.40
CHEMBL4175580 IC50 = 40000.0 nM 4.40
CHEMBL4167710 IC50 = 50000.0 nM 4.30
CHEMBL4170671 IC50 > 100000.0 nM -
CHEMBL4160038 IC50 > 100000.0 nM -
CHEMBL4161625 IC50 > 100000.0 nM -
CHEMBL73007 IC50 > 100000.0 nM -
CHEMBL3199120 IC50 > 100000.0 nM -
CHEMBL4174582 IC50 > 100000.0 nM -
CHEMBL4166666 IC50 > 100000.0 nM -